1.
Bioorg Med Chem Lett
; 19(1): 123-6, 2009 Jan 01.
Article
in English
| MEDLINE
| ID: mdl-19022669
ABSTRACT
A series of potent and selective EP(3) receptor antagonists are described. Utilizing a pharmacophore model developed for the EP(3) receptor, a series of 3,4-disubstituted indoles were shown to be high affinity ligands for this target. These compounds showed high selectivity over IP, FP and other EP receptors and are potent antagonists in functional assays.
Subject(s)
Receptors, Prostaglandin E/antagonists & inhibitors , Sulfonamides/chemical synthesis , Humans , Indoles , Ligands , Receptors, Prostaglandin E, EP3 Subtype , Structure-Activity Relationship , Sulfonamides/pharmacology
2.
Bioorg Med Chem
; 12(5): 1151-75, 2004 Mar 01.
Article
in English
| MEDLINE
| ID: mdl-14980627
ABSTRACT
A series of 3-mercapto-propionic acid derivatives that function as reversible inhibitors of carboxypeptidase U have been prepared. We present a successful design strategy using cyclic, low basicity guanidine mimetics resulting in potent, selective and bioavailable inhibitors of carboxypeptidase U (TAFIa).