Selected aryl thiosemicarbazones as a new class of multi-targeted monoamine oxidase inhibitors.

ABSTRACT: A series of 13 phenyl substituted thiosemicarbazones (SB1-SB13) were synthesized and evaluated for their inhibitory potential towards human recombinant monoamine oxidase A and B (MAO-A and MAO-B, respectively) and acetylcholinesterase. The solid state structure of SB4 was ascertained by the single X-ray diffraction technique. Compounds SB5 and SB11 were potent for MAO-A (IC₅₀ 1.82 ± 0.14) and MAO-B (IC₅₀ 0.27 ± 0.015 μM), respectively. Furthermore, SB11 showed a high selectivity index (SI > 37.0) for MAO-B. The effects of fluorine orientation revealed that SB11 (m-fluorine) showed 28.2 times higher inhibitory activity than SB12 (o-fluorine) against MAO-B. Furthermore, inhibitions by SB5 and SB11<

SUBMITTER: Mathew B 

PROVIDER: S-EPMC6254048 | biostudies-literature | 2018 Nov

REPOSITORIES: biostudies-literature