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Hypolipidemic Activity of New Phenoxyacetic Derivatives Related to α‐Asarone with Minimal Pharmacophore Features
Author(s) -
Cruz María del Carmen,
Salazar María,
Garciafigueroa Yésica,
Hernández Dolores,
Díaz Francisco,
Chamorro Germán,
Tamariz Joaquín
Publication year - 2003
Publication title -
drug development research
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 0.582
H-Index - 60
eISSN - 1098-2299
pISSN - 0272-4391
DOI - 10.1002/ddr.10281
Subject(s) - pharmacophore , chemistry , clofibrate , pharmacology , stereochemistry , drug , biological activity , chemical synthesis , structure–activity relationship , biochemistry , in vitro , biology
Five new series of potential hypolipidemic agents 3–7 were synthesized, in order to establish the minimal pharmacophore features associated to the potent hypocholesterolemic activity of natural α‐asarone ( 1 ) and synthetic clofibrate mimetic derivatives 2 . The compounds were examined in hyperlipidemic male mice after oral administration of 25, 50, and 100 mg/Kg for 6 days. The isomeric series of acids and esters 3a–3c and 4a–4c were unexpectedly less active than the most simple structural isomeric compounds 5–7 . This reveals that the phenoxyacetic acid scaffold carrying a hydrocarbon side chain, also found in derivatives 2 , seems to be the most favorable lead for further development of potent hypolipidemic drugs. Drug Dev. Res. 60:186–195, 2003. © 2003 Wiley‐Liss, Inc.