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6 results on '"Barnabas Kodasi"'

1. Adept green synthesis of Cu2O nanoparticles using Kiwi fruit (Actinidia deliciosa) juice and Studies on their cytotoxic activity and antimicrobial evaluation

Author

Barnabas Kodasi, Ravindra R. Kamble, Jayappa Manjanna, Swati R. Hoolageri, Lokesh Bheemayya, Vishwa B. Nadoni, Praveen K. Bayannavar, Shruti Dixit, Shyam Kumar Vootla, and Vijay M. Kumbar

Subjects
Cuprous oxide nanoparticles (Cu2O NPs), Antimicrobial evaluation, Cytotoxicity, Human embryonic kidney cell lines (HEK-293), Human breast cancer cell lines (MCF-7), Chemistry, QD1-999
Abstract

Background: The high-speed resistance of microbial pathogens and enfeeble of antibiotic therapy competence specifically with the rise in healthcare-associated infections (HAIs) eventually brought several thousand deaths each year. Nanoparticles have gained a lot of interest in recent years for their antibacterial and cytotoxic potential, very distinctly the copper oxide nanoparticles. Methods: Methodology involves the green synthesis of Cu2O NPs using kiwi fruit juice followed by characterization viz., XRD, SEM, UV-visible, FT-IR, particle size and zeta potential techniques. Toxicity evaluation was done by exposing HEK-293 and MCF-7 cell lines to Cu2O NPs and further testing the potency of nanoparticles against S. aureus, E.coli, A.niger and C.albicans. Results: The SEM-EDX analysis showed that Cu2O NPs are spherical in nature and pure. Half of the Cu2O NPs particles size was about 100 nm. IC50values observed for HEK-293 and MCF-7 cells were 20.51±0.52 ug mL−1and 6.25±0.27 ug mL−1. The distinct selectivity index (3.28) of the Cu2O NPS against human breast cancer cells (MCF-7) was observed. In the antimicrobial test, the zone of inhibitions were 20, 18, 14, 15 mm on S. aureus, E.coli, A.niger and C.albicans respectively. Conclusion: The Cu2O nanoparticles manifested excellent cytotoxicity against HEK-293 and MCF-7 cell lines and their antimicrobial activity was superlative with exceptional zones of inhibition against S. aureus (20 mm), E. coli (18 mm), C. albicans (14 mm) and A. niger (15 mm) revealing outstanding effectiveness at minimal concentrations.

Published
2023
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3. Coumarin-4-yl-1,2,3-triazol-4-yl-methyl-thiazolidine-2,4-diones: Synthesis, glucose uptake activity and cytotoxic evaluation

Author

Tukaram V. Metre, Barnabas Kodasi, Praveen K. Bayannavar, Lokesh Bheemayya, Vishwa B. Nadoni, Swati R. Hoolageri, Arun K. Shettar, Shrinivas D. Joshi, Vijay M. Kumbar, and Ravindra R. Kamble

Subjects
Molecular Docking Simulation, Glucose, HEK293 Cells, Diabetes Mellitus, Type 2, Coumarins, Organic Chemistry, Drug Discovery, Humans, Thiazolidines, Triazoles, Molecular Biology, Biochemistry
Abstract

Thiazolidinedione (TZD) based medications have demonstrated to enhance the insulin sensitivity control, hyperglycemia, and lipid metabolism in patients with type 2 diabetes. Hence, in this study, a new series of novel coumarin-4-yl-1,2,3-triazol-4-yl-methyl-thiazolidine-2,4-diones (TZD1-TZD18) were synthesized via copper (I)-catalyzed azide-alkyne cycloaddition "Click Chemistry". The synthesized compounds were evaluated for their glucose uptake assay and in vitro cytotoxicity against HEK-293 (human embryonic kidney) cells which were compared with the standard drug Pioglitazone. Further, molecular docking analysis of these compounds was carried out to explain the in vitro results with PPARγ (PDB ID: 3CS8) and to better understand the bonding interactions with the target protein. The outcomes of in vitro assessment, molecular docking, and pharmacokinetics of the title compounds were revealed to be highly correlated. Interestingly, the compounds TZD4, TZD10, TZD14 and TZD16 were most efficient in lowering the blood glucose level compared with standard drug.

Published
2022

5. Green synthesis of therapeutically active 1,3,4-oxadiazoles as antioxidants, selective COX-2 inhibitors and their in silico studies

Author

Vijay M. Kumbar, Barnabas Kodasi, Shyamkumar Vootla, Praveen K. Bayannavar, Aravind R. Nesaragi, Swati R. Hoolageri, Ravindra R. Kamble, Shruti Dixit, Shrinivas D. Joshi, and Jagadeesh Prasad Dasappa

Subjects
Models, Molecular, Antioxidant, Mefenamic acid, medicine.medical_treatment, In silico, Clinical Biochemistry, High selectivity, Protein Data Bank (RCSB PDB), Pharmaceutical Science, 01 natural sciences, Biochemistry, Antioxidants, chemistry.chemical_compound, Picrates, Drug Discovery, medicine, Humans, Microwaves, Molecular Biology, chemistry.chemical_classification, Oxadiazoles, Cyclooxygenase 2 Inhibitors, Molecular Structure, 010405 organic chemistry, Organic Chemistry, Biphenyl Compounds, Green Chemistry Technology, Coumarin, 0104 chemical sciences, 010404 medicinal & biomolecular chemistry, Enzyme, chemistry, Cyclooxygenase 2, Molecular Medicine, Selectivity, medicine.drug
Abstract

A modest, competent and green synthetic procedure for novel coumarinyl-1,3,4-oxadiazolyl-2-mercaptobenzoxazoles 8i-t has been reported. Analysis of the docked (PDB ID: 5IKR; A-Chain) poses of the compounds illustrated that they adopt identical conformations to the extremely selective COX-2 inhibitor. The biological outcomes as well as computational study suggested that the compounds originated to have elevated resemblance towards COX-2 enzyme than COX-1. The compounds 8i, 8l, 8q, 8r, 8s and 8t emerged as most potent and selective COX-2 inhibitors in contrast with Mefenamic acid. The selectivity index of 8l, 8n and 8r was respectively found to be 33.95, 20.25 and 24.98 which manifested their high selectivity against COX-2. Interestingly, the compounds which were active as COX-2 inhibitors were also active as antioxidant agents.

Published
2021

6. Microwave assisted regioselective synthesis of quinoline appended triazoles as potent anti-tubercular and antifungal agents via copper (I) catalyzed cycloaddition

Author

Vijay M. Kumbar, Saba Kauser J. Shaikh, Aravind R. Nesaragi, Barnabas Kodasi, Swati R. Hoolageri, Praveen K. Bayannavar, Ravindra R. Kamble, and Shrinivas D. Joshi

Subjects
Antifungal Agents, Cell Survival, Clinical Biochemistry, Protein Data Bank (RCSB PDB), Antitubercular Agents, Pharmaceutical Science, chemistry.chemical_element, Microbial Sensitivity Tests, 01 natural sciences, Biochemistry, Catalysis, chemistry.chemical_compound, Structure-Activity Relationship, Drug Discovery, Candida albicans, Humans, Microwaves, Molecular Biology, Cycloaddition Reaction, Dose-Response Relationship, Drug, Molecular Structure, 010405 organic chemistry, Organic Chemistry, Quinoline, Regioselectivity, Stereoisomerism, Mycobacterium tuberculosis, Triazoles, Copper, Combinatorial chemistry, Cycloaddition, 0104 chemical sciences, 010404 medicinal & biomolecular chemistry, Aspergillus, HEK293 Cells, chemistry, Docking (molecular), Click chemistry, Quinolines, Molecular Medicine
Abstract

Quinolin-3-yl-methyl-1,2,3-triazolyl-1,2,4-triazol-3(4H)-ones 8j-v were synthesized by click chemistry as an ultimate tactic where [3 + 2] cycloaddition of azides with terminal alkynes has been evolved. Herein, we are inclined to divulge the implication and prevalence of CuSO4·5H2O and THF/water promoted [3 + 2] cycloaddition reactions. The foremost supremacy of this method are transitory reaction times, facile workup, excellent yields (88–92%) with exorbitant purity and regioselective single product formation both under conventional and microwave method. Docking studies illustrated strong binding interactions with enzyme InhA-D148G (PDB ID: 4DQU) by means of high C-score values. The anti-tubercular and antifungal screening of synthesized compounds proclaimed promising activity. The in vitro and in silico studies imply that these triazoles appended quinolines may acquire the ideal structural prerequisites for auxiliary expansion of novel therapeutic agents.

Published
2020

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