Synthesis, evaluation and molecular modelling studies of 2-(carbazol-3-yl)-2-oxoacetamide analogues as a new class of potential pancreatic lipase inhibitors

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• 作者：S.N.C. Sridhar^a ; George Ginson^a ; P.O. Venkataramana Reddy^b ; Mukund P. Tantak^b ; Dalip Kumar^b ; ^{dalipk@pilani.bits-pilani.ac.in} ; Atish T. Paul^a ; ^{atish.paul@pilani.bits-pilani.ac.in} ; ^{paulatish@gmail.com}
• 关键词：Carbazolyl oxoacetamides ; Inhibition kinetics ; Molecular dynamics ; Orlistat ; Pancreatic lipase
• 刊名：Bioorganic & Medicinal Chemistry
• 出版年：2017
• 出版时间：15 January 2017
• 年：2017
• 卷：25
• 期：2
• 页码：609-620
• 全文大小：1389 K
• 卷排序：25

文摘

2-(Carbazol-3-yl)-2-oxoacetamide analogues were evaluated for PL inhibitory activity. Compounds 7e, 7f and 7p exhibited potential PL inhibitory activity. Probable covalent bond formation of the compounds with Ser 152 of PL was determined. Hydrophobic interactions with the lid domain played an important role in PL inhibition.