1.
Bioorg Med Chem Lett
; 17(13): 3736-40, 2007 Jul 01.
Article
in English
| MEDLINE
| ID: mdl-17467986
ABSTRACT
A series of isoxazole derivatives were synthesized and their antagonistic activities against LPA stimulation on both LPA(1)/CHO cells and rHSC cells were evaluated. Among them, 3-(4-[4-[1-(2-chloro-cyclopent-1-enyl)-ethoxycarbonylamino]-isoxazol-3- y]]-benzylsulfanyl)-propionic acid (34) showed the most potent activities.
Subject(s)
Chemistry, Pharmaceutical/methods , Isoxazoles/chemical synthesis , Lysophospholipids/antagonists & inhibitors , Animals , CHO Cells , Cell Proliferation , Cricetinae , Cricetulus , Drug Design , Fibrosis/pathology , Humans , Inhibitory Concentration 50 , Isoxazoles/chemistry , Liver/cytology , Lysophospholipids/chemistry , Propionates/chemistry , Rats
2.
Bioorg Med Chem Lett
; 13(14): 2269-72, 2003 Jul 21.
Article
in English
| MEDLINE
| ID: mdl-12824015
ABSTRACT
O-glucuronides and O-glucosides of a series of pyrazoles analogues were synthesized and evaluated for their SGLT inhibitory activity in brush border membrane vehicles (BBMVs) of rat kidney. O-glucosides of certain pyrazole analogues inhibited the transport of [(14)C]-glucose in BBMVs, and induced glucosuria in Wistar rats by intravenous injection.
