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Synthesis, in vitro enzyme activity and molecular docking studies of new benzylamine-sulfonamide derivatives as selective MAO-B inhibitors.


ABSTRACT: Many studies have been conducted on the selective inhibition of human monoamine oxidase B (hMAO-B) enzyme using benzylamine-sulphonamide derivatives. Using various chemical modifications on BB-4h, which was reported previously by our team and showed a significant level of MAO-B inhibition, novel benzylamine-sulphonamide derivatives were designed, synthesised, and their MAO inhibition potentials were evaluated. Among the tested derivatives, compounds 4i and 4t achieved IC50 values of 0.041 ± 0.001 µM and 0.065 ± 0.002 µM, respectively. The mechanism of hMAO-B inhibition by compounds 4i and 4t was studied using Lineweaver-Burk plot. The nature of inhibition was also determined to be non-competitive. Cytotoxicity tests were conducted and compounds 4i and 4t were found to be non-toxic. Molecular docking studies were also carried out for compound 4i, which was found as the most potent agent, within hMAO-B catalytic site.

SUBMITTER: Saglık BN 

PROVIDER: S-EPMC7821958 | biostudies-literature | 2020 Dec

REPOSITORIES: biostudies-literature

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Synthesis, <i>in vitro</i> enzyme activity and molecular docking studies of new benzylamine-sulfonamide derivatives as selective MAO-B inhibitors.

Sağlık Begüm Nurpelin BN   Osmaniye Derya D   Acar Çevik Ulviye U   Levent Serkan S   Kaya Çavuşoğlu Betül B   Atlı Eklioğlu Özlem Ö   Özkay Yusuf Y   Koparal Ali Savaş AS   Kaplancıklı Zafer Asım ZA  

Journal of enzyme inhibition and medicinal chemistry 20201201 1


Many studies have been conducted on the selective inhibition of human monoamine oxidase B (<i>h</i>MAO-B) enzyme using benzylamine-sulphonamide derivatives. Using various chemical modifications on <b>BB-4h</b>, which was reported previously by our team and showed a significant level of MAO-B inhibition, novel benzylamine-sulphonamide derivatives were designed, synthesised, and their MAO inhibition potentials were evaluated. Among the tested derivatives, compounds <b>4i</b> and <b>4t</b> achieved  ...[more]

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