A5018421940- Synthesis and biological activity
- Cholinesterase and Neurodegenerative Diseases
- Computational Drug Discovery Methods
- Synthesis and Biological Evaluation
- Click Chemistry and Applications
- Electrochemical sensors and biosensors
- Parkinson's Disease Mechanisms and Treatments
- SARS-CoV-2 and COVID-19 Research
- Synthesis of Organic Compounds
- Biochemical and biochemical processes
- Crystallization and Solubility Studies
- Chemical synthesis and alkaloids
- COVID-19 Clinical Research Studies
- Phytochemicals and Antioxidant Activities
- Metal complexes synthesis and properties
- Natural Antidiabetic Agents Studies
- X-ray Diffraction in Crystallography
- Chemical Synthesis and Analysis
- Free Radicals and Antioxidants
- Oxidative Organic Chemistry Reactions
- Nicotinic Acetylcholine Receptors Study
- Phenothiazines and Benzothiazines Synthesis and Activities
- COVID-19 epidemiological studies
- Synthesis and pharmacology of benzodiazepine derivatives
- Phytochemistry and Bioactive Compounds
Vinayaka Missions University
2020-2024
Chitkara University
2020
Hindu College of Pharmacy
2020
Kerala School of Mathematics
2019
Grace College & Seminary
2013-2018
University of KwaZulu-Natal
1985
The enormous burden of the COVID-19 pandemic in economic and healthcare terms has cast a shadow on serious threat antimicrobial resistance, increasing inappropriate use antibiotics shifting focus drug discovery programmes from antibacterial antifungal fields. Thus, there is pressing need for new antimicrobials involving innovative modes action (MoAs) to avoid cross-resistance rise. Thiosemicarbazones (TSCs) stand out due their easy preparation polypharmacological application, also infectious...
Abstract A series of (2 E )‐1‐(5‐bromothiophen‐2‐yl)‐3‐( para ‐substituted phenyl)prop‐2‐en‐1‐ones ( TB1 – TB11 ) was synthesized and tested for inhibitory activity toward human monoamine oxidase (hMAO). All compounds were found to be competitive, selective, reversible hMAO‐B except 2E )‐1‐(5‐bromothiophen‐2‐yl)‐3‐(4‐nitrophenyl)prop‐2‐en‐1‐one TB7 )‐1‐(5‐bromothiophen‐2‐yl)‐3‐(4‐chlorophenyl)prop‐2‐en‐1‐one TB8 ), which selective inhibitors hMAO‐A. The most potent compound,...
Abstract Numerous studies have shown that chalcones are promising scaffolds for the development of new monoamine oxidase‐B (MAO‐B) inhibitors. As a continuation our ongoing research into reversible human MAO‐B (hMAO‐B) inhibitors, two series twenty containing electron‐donating and electron‐withdrawing substituents were synthesized. All compounds found to be competitive, selective, inhibitors hMAO‐B except (2 E )‐1‐(4‐methylphenyl)‐3‐(4‐nitrophenyl)prop‐2‐en‐1‐one ( P7 )...
Abstract Two series of fluorinated chalcones containing morpholine and imidazole‐based compounds ( f1–f8 ) were synthesized evaluated for recombinant human monoamine oxidase (MAO)‐A ‐B as well acetylcholinesterase inhibitory activities. Our results indicate that are highly selective MAO‐B inhibitors having reversibility properties. All the showed weak MAO inhibitions in both isoforms. Among tested compounds, (2 E )‐3‐(3‐fluorophenyl)‐1‐[4‐(morpholin‐4‐yl)phenyl]prop‐2‐en‐1‐one f2 potent...
A series of thienylchalcones with fluoro and trifluoromethyl derivatives were synthesized evaluated for their capability to inhibit human monoamine oxidase B. The chemical structures the compounds have been ascertained by means 1HNMR, 13CNMR, mass spectroscopic data elemental analysis. results documented that these revealed moderate good inhibitory activities towards MAO-B than MAO-A. most active compound, (2E)-1-(thiophen-2-yl)-3-[4-(trifluoromethyl) phenyl] prop-2-en-1-one exhibited Ki...
A series of 13 phenyl substituted thiosemicarbazones (<bold>SB1–SB13</bold>) were synthesized and evaluated for their inhibitory potential towards human recombinant monoamine oxidase B (MAO-A MAO-B, respectively) acetylcholinesterase.
Selective monoamine oxidase-B (MAO-B) inhibitors are imperative in the treatment of various neurodegenerative disorders. Herein, we describe pharmacophore generation and atom-based three-dimensional quantitative structure-activity relationship (3D-QSAR) analyses previously reported thiophene-based hMAO-B by our research group. The aim this study was to identify principal structural features that could potentially be responsible for inhibitory activity inhibitors. best model generated...
For various neurodegenerative disorders like Alzheimer 's and Parkinson’ s diseases, selective reversible MAO ‐B inhibitors have a great therapeutic value. In our previous study, we shown that series of methoxylated chalcones with F functional group exhibited high binding affinity toward human monoamine oxidase‐B ( hMAO ‐B). continuation earlier study to extend the understanding structure–activity relationships, five new were studied for their inhibition . The results demonstrated these...
Monoamine oxidase-A and B have been studied over a long period as one of the promising drug targets for treatment depression neurodegenerative disorders. Commonly, MAO-A is associated with because its relation control serotonin levels. On other hand, MAO-B has Alzheimer's Parkinson's diseases this enzyme modulates dopamine levels in CNS. The major objective research field devoted to identify isolate selective ligands MAO-A/MAO-B so that undesirable side effects due non-selective inhibition...
Abstract The design of selective, reversible and non‐toxic hMAO−B inhibitors has received increasing attention due to their perceived utility in targeting neurological disorders like Alzheimer's Parkinson's diseases. For this purpose, herein, we report the inhibitory studies on monoamine oxidase a series ( 2E )‐1‐(2, 5‐dichlorothiophen‐3‐yl)‐3‐(4‐substitutedphenyl) prop‐2‐en‐1‐ones S1 ‐ S9 ). All compounds were found be competitive, except (2 E 4‐dichlorothiophen‐3‐yl)‐3‐(4‐nitrophenyl)...