STRUCTURE-ACTIVITY RELATIONSHIP: STUDY OF LEI-401 AS INHIBITOR OF NAPE-PLD BY PHARMACOPHORE MODELJournal: International Journal of Advanced Research (Vol.9, No. 5)
Publication Date: 2021-20-05
Authors : Nilesh S. Kadu;
Page : 662-666
Keywords : LEIâ€“401 NAPEâ€“PLD Pharmacophore Model Pyrimidine and Pyridine Scaffold Derivatives Drug Design;
N-acyl-phosphatidylethanolamine phospholipase D (NAPEÃ¢Â€Â“PLD) is considered to be the principal enzyme that produces N-acylethanolamines (NAEs), a family of signaling lipids. NAEs are involved in numerous physiological processes such as appetite, satiety, pain, inflammation, fertility, stress, and anxiety. Furthermore, aberrant NAE levels are associated with metabolic syndrome and non-alcoholic steatohepatitis (NASH). Several inhibitors for NAPEÃ¢Â€Â“PLD have been reported. But most of the inhibitors showed poor to moderate potency for NAPEÃ¢Â€Â“PLD in vitro. Recently, Mario van der Stelt et al describe the SAR of NAPEÃ¢Â€Â“PLD inhibitors that afforded LEIÃ¢Â€Â“401 in vitro. However, no attempt was instigated to produce a consensus pharmacophore model of LEIÃ¢Â€Â“401 as inhibitors of NAPEÃ¢Â€Â“PLD. Pharmacophore modeling is an efficient and useful approach to identify important patterns in a series of molecules for optimizations. The consensus pharmacophore model revealed the importance of structural features and their correlation with the biological activity.
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