Design and synthesis of lupeol analogues and their in vitro PTP-1B inhibitory activity
作者： Mohammad F. Khan , Devendra P. Mishra , E. Ramakrishna , Arun K. Rawat , Akansha Mishra
DOI: 10.1007/S00044-014-0984-2
关键词: Lupeol 、 Amide 、 Yield (chemistry) 、 Chemistry 、 Tyrosine 、 In vitro 、 Biological activity 、 Moiety 、 Carboxylic acid 、 Biochemistry 、 Stereochemistry
摘要: Synthetic analogues of the naturally occurring triterpenoid, lupeol by modification A-ring and isopropylene moiety with different carboxylic acid functionalities their biological activity were investigated. The designed considering incorporation ester amide linkages in parent molecule. They assayed for protein tyrosine phosphatase-1B (PTP-1B) inhibitory activity. Among them, compounds 9a, 9b, 14a, 14b 14c showed significant dose-dependant inhibition at 10 μM concentration. Our report is marked readily accessible synthesis, excellent yield PTP-1B effect. A synthetic approach vitro novel are described. Compounds 14a represent a new class inhibitors type 2 diabetes
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