STRUCTURE-ACTIVITY RELATIONSHIP: STUDY OF LEI-401 AS INHIBITOR OF NAPE-PLD BY PHARMACOPHORE MODEL
نویسندگان
چکیده
N-acyl-phosphatidylethanolamine phospholipase D (NAPE–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 associated with metabolic syndrome non-alcoholic steatohepatitis (NASH). Several inhibitors for NAPE–PLD have been reported. But most showed poor moderate potency vitro. Recently, Mario van der Stelt et al describe SAR afforded LEI–401 However, no attempt was instigated produce consensus pharmacophore model NAPE–PLD. Pharmacophore modeling an efficient useful approach identify important patterns series molecules optimizations. The revealed importance structural features their correlation biological activity.
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ژورنال
عنوان ژورنال: International journal of advanced research
سال: 2021
ISSN: ['2707-7802', '2707-7810']
DOI: https://doi.org/10.21474/ijar01/12889