Anton Shetnev, Julia Efimova, Olga Gasilina, Eugenia Shabalina, Sergey Baykov, Dmitry Lifanov, Elena Petersen, Mikhail Korsakov, Anél Petzer, Jacobus P. Petzer
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Monoamine oxidase inhibition by thiazole derivatives substituted with the benzenesulfonamide moiety
Based on a report that 1,3,4-oxadiazol-2-ylbenzenesulfonamides act as inhibitors of monoamine oxidase B (MAO-B), the present study explored the effect of replacing the 1,3,4-oxadiazole moiety with a 1,3-thiazole heterocycle. A series of 23 primary sulfonamides were synthesized and evaluated as in vitro inhibitors of the human MAOs. The results showed that the 1,3-thiazolylbenzenesulfonamides were specific inhibitors of MAO-B with the most potent MAO-B inhibitor presenting with an IC50 value of 0.103 µM (3j). Potent MAO-B inhibition was obtained with the substitution of the sulfonamide on the meta position of the phenyl rather than the para position. This study concluded that 1,3-thiazolylbenzenesulfonamides may serve as lead MAO inhibitors for the development of new treatments for disease states such as Parkinson’s disease.
期刊介绍：
Medicinal Chemistry Research (MCRE) publishes papers on a wide range of topics, favoring research with significant, new, and up-to-date information. Although the journal has a demanding peer review process, MCRE still boasts rapid publication, due in part, to the length of the submissions. The journal publishes significant research on various topics, many of which emphasize the structure-activity relationships of molecular biology.
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