31 results on '"Srivastava, Pavan"'
Search Results
2. ACR Appropriateness Criteria® Chronic Liver Disease
- Author
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Bashir, Mustafa R., Horowitz, Jeanne M., Kamel, Ihab R., Arif-Tiwari, Hina, Asrani, Sumeet K., Chernyak, Victoria, Goldstein, Alan, Grajo, Joseph R., Hindman, Nicole M., Kamaya, Aya, McNamara, Michelle M., Porter, Kristin K., Solnes, Lilja Bjork, Srivastava, Pavan K., Zaheer, Atif, and Carucci, Laura R.
- Published
- 2020
- Full Text
- View/download PDF
3. ACR Appropriateness Criteria® Pancreatic Cyst
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Fábrega-Foster, Kelly, Kamel, Ihab R., Horowitz, Jeanne M., Arif-Tiwari, Hina, Bashir, Mustafa R., Chernyak, Victoria, Goldstein, Alan, Grajo, Joseph R., Hindman, Nicole M., Kamaya, Aya, McNamara, Michelle M., Porter, Kristin K., Scheiman, James M., Solnes, Lilja Bjork, Srivastava, Pavan K., Zaheer, Atif, and Carucci, Laura R.
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- 2020
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4. Computational exploration and experimental validation to identify a dual inhibitor of cholinesterase and amyloid-beta for the treatment of Alzheimer’s disease
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Tripathi, Manish Kumar, Sharma, Piyoosh, Tripathi, Avanish, Tripathi, Prabhash Nath, Srivastava, Pavan, Seth, Ankit, and Shrivastava, Sushant Kumar
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- 2020
- Full Text
- View/download PDF
5. ACR Appropriateness Criteria® Right Upper Quadrant Pain
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Peterson, Christine M., McNamara, Michelle M., Kamel, Ihab R., Al-Refaie, Waddah B., Arif-Tiwari, Hina, Cash, Brooks D., Chernyak, Victoria, Goldstein, Alan, Grajo, Joseph R., Hindman, Nicole M., Horowitz, Jeanne M., Noto, Richard B., Porter, Kristin K., Srivastava, Pavan K., Zaheer, Atif, and Carucci, Laura R.
- Published
- 2019
- Full Text
- View/download PDF
6. ACR Appropriateness Criteria® Jaundice
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Hindman, Nicole M., Arif-Tiwari, Hina, Kamel, Ihab R., Al-Refaie, Waddah B., Bartel, Twyla B., Cash, Brooks D., Chernyak, Victoria, Goldstein, Alan, Grajo, Joseph R., Horowitz, Jeanne M., Kamaya, Aya, McNamara, Michelle M., Porter, Kristin K., Srivastava, Pavan K., Zaheer, Atif, and Carucci, Laura R.
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- 2019
- Full Text
- View/download PDF
7. Design and development of multitarget-directed N-Benzylpiperidine analogs as potential candidates for the treatment of Alzheimer's disease
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Sharma, Piyoosh, Tripathi, Avanish, Tripathi, Prabhash Nath, Prajapati, Santosh Kumar, Seth, Ankit, Tripathi, Manish Kumar, Srivastava, Pavan, Tiwari, Vinod, Krishnamurthy, Sairam, and Shrivastava, Sushant Kumar
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- 2019
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8. Design and development of some phenyl benzoxazole derivatives as a potent acetylcholinesterase inhibitor with antioxidant property to enhance learning and memory
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Srivastava, Pavan, Tripathi, Prabhash Nath, Sharma, Piyoosh, Rai, Sachchida Nand, Singh, Surya Pratap, Srivastava, Rakesh K., Shankar, Sharmila, and Shrivastava, Sushant K.
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- 2019
- Full Text
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9. Synthesis, evaluation and docking studies of some 4-thiazolone derivatives as effective lipoxygenase inhibitors
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Shrivastava, Sushant Kumar, Patel, Brijesh K., Tripathi, Prabhash Nath, Srivastava, Pavan, Sharma, Piyoosh, Tripathi, Avanish, Seth, Ankit, and Tripathi, Manish Kumar
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- 2018
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10. Design, synthesis, and biological evaluation of some novel indolizine derivatives as dual cyclooxygenase and lipoxygenase inhibitor for anti-inflammatory activity
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Shrivastava, Sushant K., Srivastava, Pavan, Bandresh, Robin, Tripathi, Prabhash Nath, and Tripathi, Avanish
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- 2017
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11. Design, synthesis and evaluation of some N-methylenebenzenamine derivatives as selective acetylcholinesterase (AChE) inhibitor and antioxidant to enhance learning and memory
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Shrivastava, Sushant K., Srivastava, Pavan, Upendra, T.V.R., Tripathi, Prabhash Nath, and Sinha, Saurabh K.
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- 2017
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12. Design, synthesis, evaluation and molecular modeling studies of some novel N-substituted piperidine-3-carboxylic acid derivatives as potential anticonvulsants
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Seth, Ankit, Sharma, Piyoosh A., Tripathi, Avanish, Choubey, Priyanka K., Srivastava, Pavan, Tripathi, Prabhash Nath, and Shrivastava, Sushant Kumar
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- 2018
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13. Transition to international classification of disease version 10, clinical modification: the impact on internal medicine and internal medicine subspecialties
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Caskey, Rachel N., Abutahoun, Angelos, Polick, Anne, Barnes, Michelle, Srivastava, Pavan, and Boyd, Andrew D.
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- 2018
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14. ACR Appropriateness Criteria® Liver Lesion-Initial Characterization.
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Expert Panel on Gastrointestinal Imaging, Chernyak, Victoria, Horowitz, Jeanne M, Kamel, Ihab R, Arif-Tiwari, Hina, Bashir, Mustafa R, Cash, Brooks D, Farrell, James, Goldstein, Alan, Grajo, Joseph R, Gupta, Samir, Hindman, Nicole M, Kamaya, Aya, McNamara, Michelle M, Porter, Kristin K, Solnes, Lilja Bjork, Srivastava, Pavan K, Zaheer, Atif, and Carucci, Laura R
- Abstract
Incidental liver masses are commonly identified on imaging performed for other indications. Since the prevalence of benign focal liver lesions in adults is high, even in patients with primary malignancy, accurate characterization of incidentally detected lesions is of paramount clinical importance. This document reviews utilization of various imaging modalities for characterization of incidentally detected liver lesions, discussed in the context of several clinical scenarios. For each clinical scenario, a summary of current evidence supporting the use of a given diagnostic modality is reported. The American College of Radiology Appropriateness Criteria are evidence-based guidelines for specific clinical conditions that are reviewed annually by a multidisciplinary expert panel. The guideline development and revision include an extensive analysis of current medical literature from peer reviewed journals and the application of well-established methodologies (RAND/UCLA Appropriateness Method and Grading of Recommendations Assessment, Development, and Evaluation or GRADE) to rate the appropriateness of imaging and treatment procedures for specific clinical scenarios. In those instances where evidence is lacking or equivocal, expert opinion may supplement the available evidence to recommend imaging or treatment. [ABSTRACT FROM AUTHOR]
- Published
- 2020
- Full Text
- View/download PDF
15. ACR Appropriateness Criteria® Chronic Liver Disease.
- Author
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Expert Panel on Gastrointestinal Imaging, Bashir, Mustafa R, Horowitz, Jeanne M, Kamel, Ihab R, Arif-Tiwari, Hina, Asrani, Sumeet K, Chernyak, Victoria, Goldstein, Alan, Grajo, Joseph R, Hindman, Nicole M, Kamaya, Aya, McNamara, Michelle M, Porter, Kristin K, Solnes, Lilja Bjork, Srivastava, Pavan K, Zaheer, Atif, and Carucci, Laura R
- Abstract
The liver fibrosis stage is the most important clinical determinate of morbidity and mortality in patients with chronic liver diseases. With newer therapies, liver fibrosis can be stabilized and possibly reversed, thus accurate diagnosis and staging of liver fibrosis are clinically important. Ultrasound, CT, and conventional MRI can be used to establish the diagnosis of advanced fibrosis/cirrhosis but have limited utility for assessing earlier stages of fibrosis. Elastography-based ultrasound and MRI techniques are more useful for assessment of precirrhotic hepatic fibrosis. In patients with advanced fibrosis at risk for hepatocellular carcinoma (HCC), ultrasound is the surveillance modality recommended by international guidelines in nearly all circumstances. However, in patients in whom ultrasound does not assess the liver well, including those with severe steatosis or obesity, multiphase CT or MRI may have a role in surveillance for HCC. Both multiphase CT and MRI can be used for continued surveillance in patients with a history of HCC, and contrast-enhanced ultrasound may have an emerging role in this setting. The American College of Radiology Appropriateness Criteria are evidence-based guidelines for specific clinical conditions that are reviewed annually by a multidisciplinary expert panel. The guideline development and revision include an extensive analysis of current medical literature from peer reviewed journals and the application of well-established methodologies (RAND/UCLA Appropriateness Method and Grading of Recommendations Assessment, Development, and Evaluation or GRADE) to rate the appropriateness of imaging and treatment procedures for specific clinical scenarios. In those instances where evidence is lacking or equivocal, expert opinion may supplement the available evidence to recommend imaging or treatment. [ABSTRACT FROM AUTHOR]
- Published
- 2020
- Full Text
- View/download PDF
16. ACR Appropriateness Criteria® Pancreatic Cyst.
- Author
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Expert Panel on Gastrointestinal Imaging, Fábrega-Foster, Kelly, Kamel, Ihab R, Horowitz, Jeanne M, Arif-Tiwari, Hina, Bashir, Mustafa R, Chernyak, Victoria, Goldstein, Alan, Grajo, Joseph R, Hindman, Nicole M, Kamaya, Aya, McNamara, Michelle M, Porter, Kristin K, Scheiman, James M, Solnes, Lilja Bjork, Srivastava, Pavan K, Zaheer, Atif, and Carucci, Laura R
- Abstract
Incidental pancreatic cysts are increasingly detected on imaging studies performed for unrelated indications and may be incompletely characterized on these studies. Adequate morphological characterization is critical due to the small risk of malignant degeneration associated with neoplastic pancreatic cysts, as well as the risk of associated pancreatic adenocarcinoma. For all pancreatic cysts, both size and morphology determine management. Specifically, imaging detection of features, such as pancreatic ductal communication and presence or absence of worrisome features or high-risk stigmata, have important management implications. The recommendations in this publication determine the appropriate initial imaging study to further evaluate a pancreatic cyst that was incidentally detected on a nondedicated imaging study. The recommendations are designed to maximize the yield of diagnostic information in order to better risk-stratify pancreatic cysts and assist in guiding future management. The American College of Radiology Appropriateness Criteria are evidence-based guidelines for specific clinical conditions that are reviewed annually by a multidisciplinary expert panel. The guideline development and revision include an extensive analysis of current medical literature from peer reviewed journals and the application of well-established methodologies (RAND/UCLA Appropriateness Method and Grading of Recommendations Assessment, Development, and Evaluation or GRADE) to rate the appropriateness of imaging and treatment procedures for specific clinical scenarios. In those instances where evidence is lacking or equivocal, expert opinion may supplement the available evidence to recommend imaging or treatment. [ABSTRACT FROM AUTHOR]
- Published
- 2020
- Full Text
- View/download PDF
17. Design, synthesis, and evaluation of novel N-(4-phenoxybenzyl)aniline derivatives targeting acetylcholinesterase, β-amyloid aggregation and oxidative stress to treat Alzheimer's disease.
- Author
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Srivastava, Pavan, Tripathi, Prabhash Nath, Sharma, Piyoosh, and Shrivastava, Sushant Kumar
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AMYLOID beta-protein , *ANILINE derivatives , *ALZHEIMER'S disease , *OXIDATIVE stress , *CHOLINESTERASES , *ARTIFICIAL membranes - Abstract
Novel hybrids N-(4-phenoxybenzyl)aniline were designed, synthesized, and evaluated for their potential AChE inhibitory activity along with antioxidant potential. The inhibitory potential (IC 50) of synthesized analogs was evaluated against human cholinesterases (hAChE and hBChE) using Ellman's method. Among all the tested compounds, 42 with trimethoxybenzene substituent showed maximum hAChE inhibition with the competitive type of enzyme inhibition (IC 50 = 1.32 µM; Ki = 0.879 µM). Further, parallel artificial membrane permeation assay (PAMPA-BBB) showed favorable BBB permeability by most of the synthesized compounds. Meanwhile, compound 42 also inhibited AChE-induced Aβ aggregation (39.5–66.9%) in thioflavin T assay. The in vivo behavioral studies showed dose-dependent improvement in learning and memory by compound 42. The ex vivo studies also affirmed the significant AChE inhibition and antioxidant potential of compound 42 in brain homogenates. [ABSTRACT FROM AUTHOR]
- Published
- 2019
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18. ACR Appropriateness Criteria® Right Upper Quadrant Pain.
- Author
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Expert Panel on Gastrointestinal Imaging:, Peterson, Christine M, McNamara, Michelle M, Kamel, Ihab R, Al-Refaie, Waddah B, Arif-Tiwari, Hina, Cash, Brooks D, Chernyak, Victoria, Goldstein, Alan, Grajo, Joseph R, Hindman, Nicole M, Horowitz, Jeanne M, Noto, Richard B, Porter, Kristin K, Srivastava, Pavan K, Zaheer, Atif, and Carucci, Laura R
- Abstract
Although right upper quadrant pain is a very common clinical presentation, it can be nonspecific. However, acute cholecystitis is very often the diagnosis of exclusion. This review focuses on the recommended imaging evaluation in the most commonly encountered clinical scenarios presenting with right upper quadrant abdominal pain, including suspected biliary disease, suspected acute cholecystitis, and suspected acalculous cholecystitis. This document hopes to clarify the appropriate utilization of the many imaging procedures that are available and commonly employed in these clinical settings. The American College of Radiology Appropriateness Criteria are evidence-based guidelines for specific clinical conditions that are reviewed annually by a multidisciplinary expert panel. The guideline development and revision include an extensive analysis of current medical literature from peer reviewed journals and the application of well-established methodologies (RAND/UCLA Appropriateness Method and Grading of Recommendations Assessment, Development, and Evaluation or GRADE) to rate the appropriateness of imaging and treatment procedures for specific clinical scenarios. In those instances where evidence is lacking or equivocal, expert opinion may supplement the available evidence to recommend imaging or treatment. [ABSTRACT FROM AUTHOR]
- Published
- 2019
- Full Text
- View/download PDF
19. ACR Appropriateness Criteria® Jaundice.
- Author
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Expert Panel on Gastrointestinal Imaging:, Hindman, Nicole M, Arif-Tiwari, Hina, Kamel, Ihab R, Al-Refaie, Waddah B, Bartel, Twyla B, Cash, Brooks D, Chernyak, Victoria, Goldstein, Alan, Grajo, Joseph R, Horowitz, Jeanne M, Kamaya, Aya, McNamara, Michelle M, Porter, Kristin K, Srivastava, Pavan K, Zaheer, Atif, and Carucci, Laura R
- Abstract
Jaundice is the end result of myriad causes, which makes the role of imaging in this setting particularly challenging. In the United States, the most common causes of all types of jaundice fall into four categories including hepatitis, alcoholic liver disease, blockage of the common bile duct by a gallstone or tumor, and toxic reaction to a drug or medicinal herb. Clinically, differentiating between the various potential etiologies of jaundice requires a detailed history, targeted physical examination, and pertinent laboratory studies, the results of which allow the physician to categorize the type of jaundice into mechanical or nonmechanical causes. Imaging modalities used to evaluate the jaundiced patient (all etiologies) include abdominal ultrasound (US), CT, MR cholangiopancreatography, endoscopic retrograde cholangiopancreatography and endoscopic US. The American College of Radiology Appropriateness Criteria are evidence-based guidelines for specific clinical conditions that are reviewed annually by a multidisciplinary expert panel. The guideline development and revision include an extensive analysis of current medical literature from peer reviewed journals and the application of well-established methodologies (RAND/UCLA Appropriateness Method and Grading of Recommendations Assessment, Development, and Evaluation or GRADE) to rate the appropriateness of imaging and treatment procedures for specific clinical scenarios. In those instances where evidence is lacking or equivocal, expert opinion may supplement the available evidence to recommend imaging or treatment. [ABSTRACT FROM AUTHOR]
- Published
- 2019
- Full Text
- View/download PDF
20. Design and development of novel N-(pyrimidin-2-yl)-1,3,4-oxadiazole hybrids to treat cognitive dysfunctions.
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Tripathi, Prabhash Nath, Srivastava, Pavan, Sharma, Piyoosh, Seth, Ankit, and Shrivastava, Sushant K.
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BLOOD-brain barrier , *DESIGN , *OXIDATIVE stress , *CELL lines , *MOLECULAR dynamics - Abstract
Graphical abstract Abstract Novel hybrids bearing a 2-aminopyrimidine (2-AP) moiety linked to substituted 1,3,4-oxadiazoles were designed, synthesized and biologically evaluated. Among the developed compounds, 28 noncompetitively inhibited human acetylcholinesterase (hAChE; pIC 50 = 6.52; Ki = 0.17 µM) and showed potential in vitro antioxidant activity (60.0%) when evaluated using the Ellman's and DPPH assays, respectively. Compound 28 competitively displaced propidium iodide (PI) from the peripheral anionic site (PAS) of hAChE (17.6%) and showed high blood-brain barrier (BBB) permeability, as observed in the PAMPA-BBB assay. Additionally, compound 28 inhibited hAChE-induced Aβ aggregation in a concentration-dependent manner according to the thioflavin T assay and was devoid of neurotoxic liability towards SH-SY5Y cell lines, as demonstrated by the MTT assay. The behavioral studies of compound 28 in mice showed a significant reversal of scopolamine-induced amnesia, as observed in Y-maze and passive avoidance tests. Furthermore, compound 28 exhibited significant AChE inhibition in the brain in ex vivo studies. An evaluation of oxidative stress biomarkers revealed the antioxidant potential of 28. Moreover, in silico molecular docking and dynamics simulation studies were used as a computational tool to evaluate the interactions of compound 28 with the active site residues of hAChE. [ABSTRACT FROM AUTHOR]
- Published
- 2019
- Full Text
- View/download PDF
21. Biphenyl-3-oxo-1,2,4-triazine linked piperazine derivatives as potential cholinesterase inhibitors with anti-oxidant property to improve the learning and memory.
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Tripathi, Prabhash Nath, Srivastava, Pavan, Sharma, Piyoosh, Tripathi, Manish Kumar, Seth, Ankit, Tripathi, Avanish, Rai, Sachchida Nand, Singh, Surya Pratap, and Shrivastava, Sushant K.
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ACETYLCHOLINESTERASE , *TRIAZINE derivatives , *CHOLINESTERASE inhibitors , *PROPIDIUM iodide , *MOLECULAR docking , *MOLECULAR dynamics - Abstract
Graphical abstract Highlights • Biphenyl-3-oxo-1,2,4-triazine linked piperazines were designed and synthesized. • Compound 6g significantly inhibited the AChE and showed good CNS permeability. • In vivo studies showed significant improvement in learning and memory. • Biochemical analysis showed potential antioxidant property by compound 6g. Abstract A series of novel piperazine tethered biphenyl-3-oxo-1,2,4-triazine derivatives were designed, and synthesized. Amongst the synthesized analogs, compound 6g showed significant non-competitive inhibitory potential against acetylcholinesterase (AChE, IC 50 ; 0.2 ± 0.01 μM) compared to standard donepezil (AChE, IC 50 : 0.1 ± 0.002 μM). Compound 6g also exhibited significant displacement of propidium iodide from the peripheral anionic site (PAS) of AChE (22.22 ± 1.11%) and showed good CNS permeability in PAMPA-BBB assay (P e (exp) , 6.93 ± 0.46). The in vivo behavioral studies of compound 6g indicated significant improvement in cognitive dysfunctions against scopolamine-induced amnesia mouse models. Further, ex vivo studies showed a significant AChE inhibition and reversal of the scopolamine-induced oxidative stress by compound 6g. Moreover, molecular docking and dynamics simulations of compound 6g showed a consensual binding affinity and active site interactions with the PAS and active catalytic site (CAS) residues of AChE. [ABSTRACT FROM AUTHOR]
- Published
- 2019
- Full Text
- View/download PDF
22. Quantitative Structure-activity Relationship based Design, Synthesis, and Evaluation of Novel Diarylether Derivatives as a potent Acetylcholinesterase inhibitor and Antioxidant to treat Cognitive dysfunctions.
- Author
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Srivastava, Pavan, Tripathi, Prabhash Nath, Sharma, Piyoosh, and Shrivastava, Sushant K.
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ACETYLCHOLINESTERASE inhibitors , *STRUCTURE-activity relationships , *ANTIOXIDANTS , *VITAMIN C , *ETHER derivatives , *MOLECULAR dynamics - Abstract
Some promising acetylcholinesterase (AChE) inhibitors with an antioxidant potential were designed, synthesised, and evaluated for their role in treating cognitive dysfunctions. The in silico Gaussian-based quantitative structureactivity relationship (QSAR), virtual screening (VS), QikProp drug-likeliness prediction and docking pose filtration protocols were adapted to design and screen the novel series of diaryl ether derivatives. Further, the selected compounds were investigated for their molecular binding stability using molecular dynamics (MD) simulation analysis and molecular mechanics generalised born surface area (MM-GBSA). The identified hits were synthesised and evaluated for their in vitro AChE inhibition and antioxidant potential. Among all the synthesized compounds, the compound 39 was observed as potent AChE inhibitor (AChE IC50 = 1.30 ± 0.09 μm; Ki = 0.054 ± 0.009 μM), and also the antioxidant potential of compound 39 (52.9%) was observed significantly better than standard donepezil (<10%) and parallel to ascorbic acid (56.6%). Further, compound 39 ameliorated the scopolamine-induced cognitive impairment in the Y-maze and passive avoidance testsin mice models. Ex vivo and biochemical analysis established the brain AChE inhibitory potential and antioxidant properties of compound 39. The results signified compound 39 to be a promising lead for the treatment of cognitive dysfunctions. [ABSTRACT FROM AUTHOR]
- Published
- 2019
23. Comprehensive review of mechanisms of pathogenesis involved in Alzheimer's disease and potential therapeutic strategies.
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Sharma, Piyoosh, Srivastava, Pavan, Seth, Ankit, Tripathi, Prabhash Nath, Banerjee, Anupam G., and Shrivastava, Sushant K.
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REPORTING of diseases , *ALZHEIMER'S disease , *THERAPEUTICS - Abstract
Highlights • The pathophysiological roles and underlying mechanisms of several hypotheses involved in AD are extensively reviewed. • A detailed investigation of all the conventional and novel therapeutic targets. • The identification of structural and functional motifs with a comprehensive framework of the active sites involved. • To elucidate and simplify the complexity and call for attention on the crucial areas to discover innovative therapeutics. Abstract AD is a progressive neurodegenerative disorder and a leading cause of dementia in an aging population worldwide. The enormous challenge which AD possesses to global healthcare makes it as urgent as ever for the researchers to develop innovative treatment strategies to fight this disease. An in-depth analysis of the extensive available data associated with the AD is needed for a more comprehensive understanding of underlying molecular mechanisms and pathophysiological pathways associated with the onset and progression of the AD. The currently understood pathological and biochemical manifestations include cholinergic, Aβ, tau, excitotoxicity, oxidative stress, ApoE, CREB signaling pathways, insulin resistance, etc. However, these hypotheses have been criticized with several conflicting reports for their involvement in the disease progression. Several issues need to be addressed such as benefits to cost ratio with cholinesterase therapy, the dilemma of AChE selectivity over BChE, BBB permeability of peptidic BACE-1 inhibitors, hurdles related to the implementation of vaccination and immunization therapy, and clinical failure of candidates related to newly available targets. The present review provides an insight to the different molecular mechanisms involved in the development and progression of the AD and potential therapeutic strategies, enlightening perceptions into structural information of conventional and novel targets along with the successful applications of computational approaches for the design of target-specific inhibitors. [ABSTRACT FROM AUTHOR]
- Published
- 2019
- Full Text
- View/download PDF
24. Design, synthesis, evaluation and molecular modeling studies of some novel <italic>N</italic>-substituted piperidine-3-carboxylic acid derivatives as potential anticonvulsants.
- Author
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Seth, Ankit, Sharma, Piyoosh A., Tripathi, Avanish, Choubey, Priyanka K., Srivastava, Pavan, Tripathi, Prabhash Nath, and Shrivastava, Sushant Kumar
- Abstract
Novel Schiff bases of 1-(2-Aminoethyl)piperidine-3-carboxylic acid were synthesized, characterized and screened for anticonvulsant activity. Compounds were evaluated for in vitro blood-brain barrier (BBB) permeability by parallel artificial membrane permeability BBB assay (PAMPA-BBB). Compounds
5d ,5f ,5j ,5l ,5m ,5n ,5w ,5x and5y elicited considerable in vitro permeability across BBB and further screened for in vivo anticonvulsant activity by sc-PTZ and DMCM-induced seizure models. The outcome of the in vivo models suggested that5d, 5w , and5y were most potent amongst the synthesized compounds. The neurotoxicity evaluation of5d, 5w , and5y by rotarod indicates no impairment of muscle coordination in comparison to standard diazepam. The MTT assay revealed that the test compounds (5d, 5w , and5y ) were not found to alter the cell viability considerably. In silico molecular docking and dynamics simulations were carried out on the homology modeled protein of human GABA transporter 1 (GAT1), which exhibited complementary interactions of compound5w within the active binding pocket. [ABSTRACT FROM AUTHOR]- Published
- 2018
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- View/download PDF
25. Synthesis, anti-inflammatory, analgesic, 5-lipoxygenase (5-LOX) inhibition activities, and molecular docking study of 7-substituted coumarin derivatives.
- Author
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Srivastava, Pavan, Vyas, Vivek K., Variya, Bhavesh, Patel, Palak, Qureshi, Gulamnizami, and Ghate, Manjunath
- Subjects
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ANTI-inflammatory agents , *LIPOXYGENASES , *ENZYME inhibitors , *COUMARIN derivatives , *MOLECULAR docking , *DRUG synthesis - Abstract
In the present study, 7-subsituted coumarin derivatives were synthesized using various aromatic and heterocyclic amines, and evaluated in vivo for anti-inflammatory and analgesic activity, and for ulcerogenic risk. The most active compounds were evaluated in vitro for 5-lipoxygenase (5-LOX) inhibition. Docking study was performed to predict the binding affinity, and orientation at the active site of the enzyme. In vivo anti-inflammatory and analgesic activity, and in vitro 5-LOX enzyme inhibition study revealed that compound 33 and 35 are the most potent compounds in all the screening methods. In vitro kinetic study of 35 showed mixed or non-competitive type of inhibition with 5-LOX enzyme. Presence of OCH 3 group in 35 and Cl in 33 at C6-position of benzothiazole ring were found very important substitutions for potent activity. [ABSTRACT FROM AUTHOR]
- Published
- 2016
- Full Text
- View/download PDF
26. Feasibility of Inpatient Continuous Glucose Monitoring During the COVID-19 Pandemic: Early Experience.
- Author
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Reutrakul, Sirimon, Genco, Matthew, Salinas, Harley, Sargis, Robert M., Paul, Carlie, Eisenberg, Yuval, Fang, Jiali, Caskey, Rachel N., Henkle, Sarah, Fatoorehchi, Sam, Osta, Amanda, Srivastava, Pavan, Johnson, Alexia, Messmer, Sarah E., Barnes, Michelle, Pratuangtham, Sarida, and Layden, Brian T.
- Subjects
COVID-19 pandemic ,GLUCOSE ,BLOOD sugar monitoring ,PERSONAL protective equipment - Abstract
The article focuses on continuous glucose monitoring (CGM) systems have been explored in a few studies for non–intensive care unit (ICU) patients. Topics include the COVID-19 pandemic has shortage of personal protective equipment (PPE) became a concern, and the U.S. Food and Drug Administration has announced it would not object to the use of CGM systems to assist with COVID-19 patient monitoring.
- Published
- 2020
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27. ACR Appropriateness Criteria® Staging of Pancreatic Ductal Adenocarcinoma.
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Qayyum, Aliya, Tamm, Eric P., Kamel, Ihab R., Allen, Peter J., Arif-Tiwari, Hina, Chernyak, Victoria, Gonda, Tamas A., Grajo, Joseph R., Hindman, Nicole M., Horowitz, Jeanne M., Kaur, Harmeet, McNamara, Michelle M., Noto, Richard B., Srivastava, Pavan K., Lalani, Tasneem, and Expert Panel on Gastrointestinal Imaging:
- Abstract
Pancreatic adenocarcinoma is associated with poor overall prognosis. Complete surgical resection is the only possible option for cure. As such, increasingly complex surgical techniques including sophisticated vascular reconstruction are being used. Continued advances in surgical techniques, in conjunction with use of combination systemic therapies, and radiation therapy have been suggested to improve outcomes. A key aspect to surgical success is reporting of pivotal findings beyond absence of distant metastases, such as tumor size, location, and degree of tumor involvement of specific vessels associated with potential perineural tumor spread. Multiphase contrast-enhanced multidetector CT and MRI are the imaging modalities of choice for pretreatment staging and presurgical determination of resectability. Imaging modalities such as endoscopic ultrasound and fluorine-18-2-fluoro-2-deoxy-D-glucose imaging with PET/CT are indicated for specific scenarios such as biopsy guidance and confirmation of distant metastases, respectively. The American College of Radiology Appropriateness Criteria are evidence-based guidelines for specific clinical conditions that are reviewed annually by a multidisciplinary expert panel. The guideline development and revision include an extensive analysis of current medical literature from peer reviewed journals and the application of well-established methodologies (RAND/UCLA Appropriateness Method and Grading of Recommendations Assessment, Development, and Evaluation or GRADE) to rate the appropriateness of imaging and treatment procedures for specific clinical scenarios. In those instances where evidence is lacking or equivocal, expert opinion may supplement the available evidence to recommend imaging or treatment. [ABSTRACT FROM AUTHOR]
- Published
- 2017
- Full Text
- View/download PDF
28. Design and development of novel p-aminobenzoic acid derivatives as potential cholinesterase inhibitors for the treatment of Alzheimer's disease.
- Author
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Shrivastava, Sushant K., Sinha, Saurabh K., Srivastava, Pavan, Tripathi, Prabhash N., Sharma, Piyoosh, Tripathi, Manish K., Tripathi, Avanish, Choubey, Priyanka K., Waiker, Digambar K., Aggarwal, Lalit M., Dixit, Manish, Kheruka, Subhash C., Gambhir, Sanjay, Shankar, Sharmila, and Srivastava, Rakesh K.
- Subjects
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AMINOBENZOIC acids , *ACETYLCHOLINESTERASE , *BUTYRYLCHOLINESTERASE , *CHOLINESTERASE inhibitors , *ALZHEIMER'S disease treatment - Abstract
Graphical abstract Highlights • Novel p-aminobenzoic acid derivatives were designed, synthesized and characterized. • The compounds exhibited significant inhibitory potential against AChE and BChE. • Compound 22 exhibited significant improvements in working and reference memory. • The ex vivo study confirmed the ability of compound 22 to cross the BBB. • The in silico studies demonstrated the binding to active pocket in a stable manner. Abstract Based on the quantitative structure-activity relationship (QSAR), some novel p-aminobenzoic acid derivatives as promising cholinesterase enzyme inhibitors were designed, synthesized, characterized and evaluated to enhance learning and memory. The in vitro enzyme kinetic study of the synthesized compounds revealed the type of inhibition on the respective acetylcholinesterase (AChE) and butyrylcholinesterase (BChE) enzymes. The in vivo studies of the synthesized compounds exhibited significant reversal of cognitive deficits in the animal models of amnesia as compared to standard drug donepezil. Further, the ex vivo studies in the specific brain regions like the hippocampus, hypothalamus, and prefrontal cortex regions also exhibited AChE inhibition comparable to standard donepezil. The in silico molecular docking and dynamics simulations studies of the most potent compound 22 revealed the consensual interactions at the active site pocket of the AChE. [ABSTRACT FROM AUTHOR]
- Published
- 2019
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29. Design and development of 1,3,4-oxadiazole derivatives as potential inhibitors of acetylcholinesterase to ameliorate scopolamine-induced cognitive dysfunctions.
- Author
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Mishra, Puja, Sharma, Piyoosh, Tripathi, Prabhash Nath, Gupta, Sukesh Kumar, Srivastava, Pavan, Seth, Ankit, Tripathi, Avanish, Krishnamurthy, Sairam, and Shrivastava, Sushant Kumar
- Subjects
- *
ACETYLCHOLINESTERASE inhibitors , *ACETYLCHOLINESTERASE , *CHOLINESTERASES , *ARTIFICIAL membranes , *MOLECULAR hybridization , *PERMEABILITY - Abstract
• 4-AP tethered 1,3,4-oxadiazole derivatives were designed and synthesized. • Compound 9 elicited significant non-competitive type of hAChE inhibition. • Compound 9 showed significant brain permeability in PAMPA-BBB assay. • Compound 9 ameliorated scopolamine- induced cognitive impairment in mice models. • Biochemical analysis using brain homogenates suggested antioxidant activity by 9. The novel hybrids bearing 4-aminopyridine (4-AP) tethered with substituted 1,3,4-oxadiazole nucleus were designed, synthesized, and evaluated for their potential AChE inhibitory property along with significant antioxidant potential. The inhibitory potential (IC 50) of synthesized analogs was evaluated against human cholinesterases (hAChE and hBChE) using Ellman's method. Among all the compounds, 9 with 4-hydroxyl substituent showed maximum hAChE inhibition with the non-competitive type of enzyme inhibition (IC 50 = 1.098 µM; Ki = 0.960 µM). Further, parallel artificial membrane permeation assay (PAMPA-BBB) showed significant BBB permeability in most of the synthesized compounds. Meanwhile, compound 9 also inhibited AChE-induced Aβ aggregation (38.2–65.9%) by thioflavin T assay. The in vivo behavioral studies showed dose-dependent improvement in learning and memory by compound 9. The ex vivo studies also affirmed the significant AChE inhibition and antioxidant potential of compound 9 in brain homogenates. [ABSTRACT FROM AUTHOR]
- Published
- 2019
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30. Design, Synthesis, Evaluation and Computational Studies of Nipecotic Acid-Acetonaphthone Hybrids as Potential Antiepileptic Agents.
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Seth A, Sharma PA, Tripathi A, Choubey PK, Srivastava P, Tripathi PN, and Shrivastava SK
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- Animals, Anticonvulsants chemical synthesis, Anticonvulsants chemistry, Blood-Brain Barrier metabolism, Disease Models, Animal, Drosophila, Drug Design, Female, GABA Plasma Membrane Transport Proteins chemistry, GABA Uptake Inhibitors chemical synthesis, GABA Uptake Inhibitors chemistry, GABA Uptake Inhibitors therapeutic use, Humans, Hydrophobic and Hydrophilic Interactions, Male, Mice, Molecular Docking Simulation, Molecular Dynamics Simulation, Naphthalenes chemical synthesis, Naphthalenes chemistry, Nipecotic Acids chemical synthesis, Nipecotic Acids chemistry, Tiagabine, Anticonvulsants therapeutic use, Epilepsy drug therapy, Naphthalenes therapeutic use, Nipecotic Acids therapeutic use
- Abstract
Background: Nipecotic acid is considered to be one of the most potent inhibitors of neuronal and glial γ-aminobutyric acid (GABA) uptake in vitro. However, nipecotic acid does not readily cross the blood-brain barrier (BBB) following peripheral administration, owing to its hydrophilic nature., Objective: A series of substituted acetonaphthones tethered nipecotic acid derivatives were designed and synthesized with an aim to improve the lipophilicity and the blood-brain barrier (BBB) permeation., Methods: Synthesized compounds were tested in mice models of PTZ, pilocarpine, and DMCM induced epilepsy, in vivo. The rota-rod test was performed to determine the acute neurotoxicity of the potential leads (4a, 4b, and 4i). These potential hybrids were also evaluated for their ability to cross the BBB by an in vitro parallel artificial membrane permeability BBB assay (PAMPA-BBB). The leads were subjected to in silico molecular docking and dynamics studies on homology modelled protein of human GABA (γ-amino butyric acid) transporter 1 (GAT1) and prediction of their pharmacokinetic properties., Result: Amongst the synthesized derivatives, compounds 3a, 3b, 3i, 4a, 4b, and 4i exhibited increased latency of seizures against subcutaneous pentylenetetrazole (scPTZ) induced seizures in mice. Derivatives 4a, 4b, 4i were more effective compared to nipecotic acid ester counterparts 3a, 3b and 3i placing the importance of the presence of free carboxyl group in the centre. The findings revealed that 4i was comparatively more permeable (Pe= 8.89) across BBB than the standard tiagabine (Pe= 7.86). In silico studies proved the consensual interactions of compound 4i with the active binding pocket., Conclusion: Some nipecotic acid-acetonaphthone hybrids with considerable anti-epileptic activity, drug like properties and the ability to permeate the BBB have been successfully synthesized., (Copyright© Bentham Science Publishers; For any queries, please email at epub@benthamscience.org.)
- Published
- 2018
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31. ACR Appropriateness Criteria ® Staging of Pancreatic Ductal Adenocarcinoma.
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Qayyum A, Tamm EP, Kamel IR, Allen PJ, Arif-Tiwari H, Chernyak V, Gonda TA, Grajo JR, Hindman NM, Horowitz JM, Kaur H, McNamara MM, Noto RB, Srivastava PK, and Lalani T
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- Adenocarcinoma surgery, Carcinoma, Pancreatic Ductal surgery, Evidence-Based Medicine, Humans, Neoplasm Staging, Pancreatic Neoplasms surgery, Prognosis, Societies, Medical, United States, Adenocarcinoma diagnostic imaging, Adenocarcinoma pathology, Carcinoma, Pancreatic Ductal diagnostic imaging, Carcinoma, Pancreatic Ductal pathology, Diagnostic Imaging methods, Pancreatic Neoplasms diagnostic imaging, Pancreatic Neoplasms pathology
- Abstract
Pancreatic adenocarcinoma is associated with poor overall prognosis. Complete surgical resection is the only possible option for cure. As such, increasingly complex surgical techniques including sophisticated vascular reconstruction are being used. Continued advances in surgical techniques, in conjunction with use of combination systemic therapies, and radiation therapy have been suggested to improve outcomes. A key aspect to surgical success is reporting of pivotal findings beyond absence of distant metastases, such as tumor size, location, and degree of tumor involvement of specific vessels associated with potential perineural tumor spread. Multiphase contrast-enhanced multidetector CT and MRI are the imaging modalities of choice for pretreatment staging and presurgical determination of resectability. Imaging modalities such as endoscopic ultrasound and fluorine-18-2-fluoro-2-deoxy-D-glucose imaging with PET/CT are indicated for specific scenarios such as biopsy guidance and confirmation of distant metastases, respectively. The American College of Radiology Appropriateness Criteria are evidence-based guidelines for specific clinical conditions that are reviewed annually by a multidisciplinary expert panel. The guideline development and revision include an extensive analysis of current medical literature from peer reviewed journals and the application of well-established methodologies (RAND/UCLA Appropriateness Method and Grading of Recommendations Assessment, Development, and Evaluation or GRADE) to rate the appropriateness of imaging and treatment procedures for specific clinical scenarios. In those instances where evidence is lacking or equivocal, expert opinion may supplement the available evidence to recommend imaging or treatment., (Copyright © 2017 American College of Radiology. Published by Elsevier Inc. All rights reserved.)
- Published
- 2017
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