Yl. Wang et al., The synthesis and human FP receptor binding affinity of 13,14-dihydro prostaglandin F-1 alpha sulfonamides: Potential treatments for osteoporosis, CHEM PHARM, 48(9), 2000, pp. 1332-1337
A novel class of saturated prostaglandin F-2 alpha sulfonamide analogs have
been synthesized and evaluated in the human FP receptor binding assay for
potential use in the treatment of osteoporosis. These compounds have been m
odified at the C-1 carboxylic acid moiety and at the C-16-C-20 region of th
e prostaglandin, Based on the structure-activity relationships, it was foun
d that at C-1, the aryl sulfonamide analogs possessed greater affinity for
the hFP receptor when compared to alkyl sulfonamides. When the sulfonamide
was introduced into the C-16-C-20 region (omega chain) of the prostaglandin
, a significant reduction in binding a as observed. These results are discu
ssed within the framework of a proposed model for the human FP receptor.