Secci, Daniela published the artcile4-(3-Nitrophenyl)thiazol-2-ylhydrazone derivatives as antioxidants and selective hMAO-B inhibitors: synthesis, biological activity and computational analysis, Category: benzothiophene, the main research area is nitrophenylthiazolyl hydrazone synthesis antioxidant monoamine oxidase neurodegenerative disorder; (Thiazol-2-yl)hydrazone derivatives; Alzheimer’s disease; Parkinson’s disease; antioxidants; inhibitor; molecular modelling; monoamine oxidase; selective.
A new series of 4-(3-nitrophenyl)thiazol-2-ylhydrazone derivatives were designed, synthesized, 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 biol. testing demonstrated that the presence of the hydrazothiazole nucleus bearing at C4 a Ph 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 mol. modeling studies provided insight into the multiple interactions and structural requirements for the reported MAO inhibitory properties.
Journal of Enzyme Inhibition and Medicinal Chemistry published new progress about Alzheimer disease. 1468-83-3 belongs to class benzothiophene, name is 3-Acetylthiophene, and the molecular formula is C6H6OS, Category: benzothiophene.
Referemce:
Benzothiophene – Wikipedia,
Benzothiophene | C8H6S – PubChem