7 results on '"Carradori S"'
Search Results
2. The State of the Art of Pyrazole Derivatives as Monoamine Oxidase Inhibitors and Antidepressant/Anticonvulsant Agents
- Author
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Secci, D., primary, Bolasco, A., additional, Chimenti, P., additional, and Carradori, S., additional
- Published
- 2011
- Full Text
- View/download PDF
3. New Aspects of Monoamine Oxidase B Inhibitors: The Key Role of Halogens to Open the Golden Door.
- Author
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Mathew B, Carradori S, Guglielmi P, Uddin MS, and Kim H
- Subjects
- Chromones, Halogens, Humans, Monoamine Oxidase Inhibitors pharmacology, Structure-Activity Relationship, Monoamine Oxidase metabolism
- Abstract
A large plethora of drugs and promising lead compounds contain halogens in their structures. The introduction of such moieties strongly modulates their physical-chemical features as well as pharmacokinetic and pharmacodynamic profile. The most important outcome was shown to be the ability of these halogens to favourably influence the drug-target interaction and energetic stability within the active site by the establishment of halogen bonds. This review attempted to demonstrate the key role exerted by these versatile moieties when correctly located in an organic scaffold to display Monoamine Oxidase (MAO) inhibition and selectivity towards the B isoform of this important enzyme. Human MAOs are well-recognized as therapeutic targets for mood disorders and neurodegenerative diseases and medicinal chemists were prompted to discover the structural requirements crucial to discriminate the slight differences between the active sits of the two isoforms (MAO-A and MAOB). The analysis of the structure-activity relationships of the most important scaffolds (hydrazothiazoles, coumarins, chromones, chalcones, pyrazolines) and the impact of halogen (F, Cl, Br and I) insertion on this biological activity and isozyme selectivity have been reported being a source of inspiration for the medicinal chemists., (Copyright© Bentham Science Publishers; For any queries, please email at epub@benthamscience.net.)
- Published
- 2021
- Full Text
- View/download PDF
4. The Chronicle of COVID-19 and Possible Strategies to Curb the Pandemic.
- Author
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Kumar R, Harilal S, Al-Sehemi AG, Mathew GE, Carradori S, and Mathew B
- Subjects
- Antiviral Agents pharmacology, Antiviral Agents therapeutic use, Communicable Disease Control, Humans, SARS-CoV-2, COVID-19, Pandemics prevention & control
- Abstract
COVID-19, a type of infection that emerged in Wuhan, has become a pandemic affecting people worldwide and is rapidly spreading and evolving. Day by day, the confirmed cases and deaths are increasing many folds. SARS-CoV-2 is a novel virus; therefore, limited data are available to curb the disease. Epidemiological approaches, such as isolation, quarantine, social distancing, lockdown, and curfew, are being employed to halt the spread of the disease. Individual and joint efforts all over the world are producing a wealth of data and information which are expected to produce therapeutic strategies against COVID-19. Current research focuses on the utilization of antiviral drugs, repurposing strategies, vaccine development, as well as basic to advanced research about the organism and the infection. The review focuses on its life cycle, targets, and possible therapeutic strategies, which can lead to further research and development of COVID-19 therapy., (Copyright© Bentham Science Publishers; For any queries, please email at epub@benthamscience.net.)
- Published
- 2021
- Full Text
- View/download PDF
5. A Comprehensive Overview of Colon Cancer- A Grim Reaper of the 21st Century.
- Author
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Kumar R, Harilal S, Carradori S, and Mathew B
- Subjects
- Biomarkers, Tumor, Humans, Mass Screening, Colonic Neoplasms, Colorectal Neoplasms diagnosis, Colorectal Neoplasms drug therapy, Gastrointestinal Microbiome
- Abstract
A few decades ago, the incidence of colorectal cancer (CRC) was low and is now the fourth in the list of deadly cancers producing nearly a million deaths annually. A population that is aging along with risk factors such as smoking, obesity, sedentary lifestyle with little or no physical activity, and non-healthy food habits of developed countries can increase the risk of colorectal cancer. The balance in gut microbiota and the metabolites produced during bacterial fermentation within the host plays a significant role in regulating intestinal diseases as well as colorectal cancer development. Recent progress in the understanding of illness resulted in multiple treatment options such as surgery, radiation, and chemotherapy, including targeted therapy and multitherapies. The treatment plan for CRC depends on the location, stage and grade of cancer as well as genomic biomarker tests. Despite all the advancements made in the genetic and molecular aspects of the disease, the knowledge seems inadequate as the drug action as well as the wide variation in drug response did not appear strongly correlated with the individual molecular and genetic characteristics, which suggests the requirement of comprehensive molecular understanding of this complex heterogeneous disease. Furthermore, multitherapies or a broad spectrum approach, which is an amalgamation of the various promising as well as effective therapeutic strategies that can tackle heterogeneity and act on several targets of the disease, need to be validated in clinical studies. The latest treatment options have significantly increased the survival of up to three years in the case of advanced disease. The fact that colorectal cancer is developed from a polypoid precursor, as well as the symptoms of the disease that occur at an advanced stage, underlines how screening programs can help early detection and decrease mortality as well as morbidity from CRC., (Copyright© Bentham Science Publishers; For any queries, please email at epub@benthamscience.net.)
- Published
- 2021
- Full Text
- View/download PDF
6. Targeting Malassezia species for Novel Synthetic and Natural Antidandruff Agents.
- Author
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Angiolella L, Carradori S, Maccallini C, Giusiano G, and Supuran CT
- Subjects
- Antifungal Agents chemical synthesis, Antifungal Agents chemistry, Biological Products chemical synthesis, Biological Products chemistry, Carbonic Anhydrases metabolism, Enzyme Inhibitors chemical synthesis, Enzyme Inhibitors chemistry, Lipase antagonists & inhibitors, Lipase metabolism, Microbial Sensitivity Tests, Antifungal Agents pharmacology, Biological Products pharmacology, Dandruff drug therapy, Dandruff microbiology, Enzyme Inhibitors pharmacology, Malassezia drug effects
- Abstract
Malassezia spp. are lipophilic yeasts not only present in the normal skin microflora, but also responsible of skin-related diseases (pityriasis versicolor, seborrheic/atopic dermatitis and dandruff) as well as systemic fungal infections in humans and animals. Their treatment and eradication are mainly based on old azole drugs, which are characterized by poor compliance, unpredictable clinical efficacy, emerging resistance and several side effects. These drawbacks have prompted the research toward novel synthetic and natural derivatives/ nanomaterials targeting other pivotal enzymes/pathways such as carbonic anhydrase (MgCA) and lipases, alone or in combination, in order to improve the eradication rate of this fungus. This review accomplished an update on this important topic dealing with the latest discoveries of synthetic scaffolds and natural products for the treatment of Malassezia spp.-related diseases, thus suggesting new opportunities to design innovative and alternative anti-dandruff drugs., (Copyright© Bentham Science Publishers; For any queries, please email at epub@benthamscience.org.)
- Published
- 2017
- Full Text
- View/download PDF
7. Dual Cyclooxygenase and Carbonic Anhydrase Inhibition by Nonsteroidal Anti-Inflammatory Drugs for the Treatment of Cancer.
- Author
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De Monte C, Carradori S, Gentili A, Mollica A, Trisciuoglio D, and Supuran CT
- Subjects
- Animals, Humans, Anti-Inflammatory Agents, Non-Steroidal pharmacology, Anti-Inflammatory Agents, Non-Steroidal therapeutic use, Carbonic Anhydrase Inhibitors pharmacology, Carbonic Anhydrase Inhibitors therapeutic use, Cyclooxygenase 2 Inhibitors pharmacology, Cyclooxygenase 2 Inhibitors therapeutic use, Neoplasms drug therapy, Sulfonamides pharmacology, Sulfonamides therapeutic use
- Abstract
Among the class of nonsteroidal anti-inflammatory drugs (NSAIDs), COX-2 inhibitors or "coxibs" selectively inhibit the activity of the inducible isoform of cyclooxygenase. Moreover, there is emerging evidence that the sulfonamide-type coxibs, but not the methylsulfones, display an inhibitory activity also against several isoforms of human carbonic anhydrase (CA, EC 4.2.1.1). In this regard, celecoxib and valdecoxib, possessing a primary sulfonamide that binds to the zinc ion at the active site of the enzyme, are nanomolar inhibitors of the cancer-related hCA IX isoform. Also meloxicam and lornoxicam, NSAIDs belonging to the class of "oxicams", that contain a cyclic tertiary sulfonamide moiety, inhibit this isoform at low micromolar concentrations. The multiple pharmacological effects of the sulfonamide anti-inflammatory agents could be ascribed to the dual inhibition of CA and COX enzymes, supporting the evidence that inflammation and hypoxia pathways are involved in cancer onset and progression and suggesting that the antitumoral activity of these compounds should be further explored for their possible use in the polypharmacology of cancer prevention and therapy.
- Published
- 2015
- Full Text
- View/download PDF
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