Analgesic and Anticancer Activity of Benzoxazole Clubbed 2-Pyrrolidinones as Novel Inhibitors of Monoacylglycerol Lipase.

ABSTRACT: Ten benzoxazole clubbed 2-pyrrolidinones (11-20) as human monoacylglycerol lipase inhibitors were designed on the criteria fulfilling the structural requirements and on the basis of previously reported inhibitors. The designed, synthesized, and characterized compounds (11-20) were screened against monoacylglycerol lipase (MAGL) in order to find potential inhibitors. Compounds 19 (4-NO₂ derivative) and 20 (4-SO₂NH₂ derivative), with an IC₅₀ value of 8.4 and 7.6 nM, were found most active, respectively. Both of them showed micromolar potency (IC₅₀ value above 50 µM) against a close analogue, fatty acid amide hydrolase (FAAH), therefore considered as selective inhibitors of MAGL. Molecular docking

SUBMITTER: Afzal O 

PROVIDER: S-EPMC8074287 | biostudies-literature | 2021 Apr

REPOSITORIES: biostudies-literature