Novel 1,3,4-thiadiazole compounds as potential MAO-A inhibitors - design, synthesis, biological evaluation and molecular modelling.

ABSTRACT: Monoamine oxidases (MAOs) are important drug targets for the management of neurological disorders. Herein, a series of new 1,3,4-thiadiazole derivatives bearing various alkyl/arylamine moieties as MAO inhibitors were designed and synthesized. All of the compounds were more selective against hMAO-A than hMAO-B. The half maximal inhibitory concentration (IC₅₀) values of most of the compounds were lower than that of the common drug moclobemide (IC₅₀ = 4.664 μM) and compound 6b was proven to be the most active compound (IC₅₀ = 0.060 μM). Moreover, it was seen that compound 6b showed a similar inhibition profile to that of clorgyline (IC₅₀ = 0.048 μM). The inhibition profile was found to be reversible and competitive for co

SUBMITTER: Saglık BN 

PROVIDER: S-EPMC7513386 | biostudies-literature | 2020 Sep

REPOSITORIES: biostudies-literature