4-(3-Nitrophenyl)thiazol-2-ylhydrazone derivatives as antioxidants and selective hMAO-B inhibitors: synthesis, biological activity and computational analysis
Copyright policy )4-(3-Nitrophenyl)thiazol-2-ylhydrazone derivatives as antioxidants and selective hMAO-B inhibitors: synthesis, biological activity and computational analysis
A new series of 4-(3-nitrophenyl)thiazol-2-ylhydrazone derivatives were designed, synthesised, and evaluated to assess their inhibitory effect on the human monoamine oxidase (hMAO) A and B isoforms. Different (un)substituted (hetero)aromatic substituents were linked to N1 of the hydrazone in order to establish robust structure-activity relationships. The results of the biological testing demonstrated that the presence of the hydrazothiazole nucleus bearing at C4 a phenyl ring functionalised at the meta position with a nitro group represents an important pharmacophoric feature to obtain selective and reversible human MAO-B inhibition for the treatment of neurodegenerative disorders. In addition, the most potent and selective MAO-B inhibitors were evaluated in silico as potential cholinesterase (AChE/BuChE) inhibitors and in vitro for antioxidant activities. The results obtained from molecular modelling studies provided insight into the multiple interactions and structural requirements for the reported MAO inhibitory properties.
- Roma Tre University Italy
- Selçuk University Turkey
- Sapienza University of Rome Italy
- University of Chieti-Pescara Italy
- Magna Graecia University Italy
Models, Molecular, Inhibitor, Monoamine Oxidase Inhibitors, parkinson’s disease, Parkinson's disease, RM1-950, Selective, Antioxidants, selective, Humans, monoamine oxidase, Monoamine Oxidase, (Thiazol-2-yl)hydrazone derivatives, (thiazol-2-yl)hydrazone derivatives; Alzheimer’s disease; antioxidants; inhibitor; molecular modelling; monoamine oxidase; Parkinson’s disease; selective; acetylcholinesterase; antioxidants; butyrylcholinesterase; cholinesterase inhibitors; humans; hydrazones; models, molecular; molecular structure; monoamine oxidase; monoamine oxidase inhibitors; thiazoles;, Molecular Structure, Monoamine oxidase, Hydrazones, alzheimer’s disease, Alzheimer's disease, molecular modelling, inhibitor, Thiazoles, antioxidants, Butyrylcholinesterase, Parkinson’s disease, Acetylcholinesterase, (Thiazol-2-yl)hydrazone derivatives; Alzheimer’s disease; antioxidants; inhibitor; molecular modelling; monoamine oxidase; Parkinson’s disease; selective; Acetylcholinesterase; Antioxidants; Butyrylcholinesterase; Cholinesterase Inhibitors; Humans; Hydrazones; Models, Molecular; Molecular Structure; Monoamine Oxidase; Monoamine Oxidase Inhibitors; Thiazoles; Pharmacology; Drug Discovery3003 Pharmaceutical Science, (thiazol-2-yl)hydrazone derivatives, Molecular modelling, Therapeutics. Pharmacology, Cholinesterase Inhibitors, Alzheimer’s disease, Research Paper
Models, Molecular, Inhibitor, Monoamine Oxidase Inhibitors, parkinson’s disease, Parkinson's disease, RM1-950, Selective, Antioxidants, selective, Humans, monoamine oxidase, Monoamine Oxidase, (Thiazol-2-yl)hydrazone derivatives, (thiazol-2-yl)hydrazone derivatives; Alzheimer’s disease; antioxidants; inhibitor; molecular modelling; monoamine oxidase; Parkinson’s disease; selective; acetylcholinesterase; antioxidants; butyrylcholinesterase; cholinesterase inhibitors; humans; hydrazones; models, molecular; molecular structure; monoamine oxidase; monoamine oxidase inhibitors; thiazoles;, Molecular Structure, Monoamine oxidase, Hydrazones, alzheimer’s disease, Alzheimer's disease, molecular modelling, inhibitor, Thiazoles, antioxidants, Butyrylcholinesterase, Parkinson’s disease, Acetylcholinesterase, (Thiazol-2-yl)hydrazone derivatives; Alzheimer’s disease; antioxidants; inhibitor; molecular modelling; monoamine oxidase; Parkinson’s disease; selective; Acetylcholinesterase; Antioxidants; Butyrylcholinesterase; Cholinesterase Inhibitors; Humans; Hydrazones; Models, Molecular; Molecular Structure; Monoamine Oxidase; Monoamine Oxidase Inhibitors; Thiazoles; Pharmacology; Drug Discovery3003 Pharmaceutical Science, (thiazol-2-yl)hydrazone derivatives, Molecular modelling, Therapeutics. Pharmacology, Cholinesterase Inhibitors, Alzheimer’s disease, Research Paper
citations This is an alternative to the "Influence" indicator, which also reflects the overall/total impact of an article in the research community at large, based on the underlying citation network (diachronically).47 popularity This indicator reflects the "current" impact/attention (the "hype") of an article in the research community at large, based on the underlying citation network.Top 10% influence This indicator reflects the overall/total impact of an article in the research community at large, based on the underlying citation network (diachronically).Top 10% impulse This indicator reflects the initial momentum of an article directly after its publication, based on the underlying citation network.Top 1%
Citations provided by BIP!Popularity provided by BIP!