TY - JOUR
T1 - Hypolipidemic Activity of New Phenoxyacetic Derivatives Related to α-Asarone with Minimal Pharmacophore Features
AU - Del Carmen Cruz, María
AU - Salazar, María
AU - Garciafigueroa, Yésica
AU - Hernández, Dolores
AU - Díaz, Francisco
AU - Chamorro, Germán
AU - Tamariz, Joaquín
PY - 2003/11
Y1 - 2003/11
N2 - 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.
AB - 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.
KW - Hypocholesterolemia
KW - Minimal pharmacophores
KW - Phenoxyacetic scaffold
KW - α-asarone
UR - http://www.scopus.com/inward/record.url?scp=0242299718&partnerID=8YFLogxK
U2 - 10.1002/ddr.10281
DO - 10.1002/ddr.10281
M3 - Artículo
SN - 0272-4391
VL - 60
SP - 186
EP - 195
JO - Drug Development Research
JF - Drug Development Research
IS - 3
ER -