The synthesis and human FP receptor binding affinity of 13,14-dihydro prostaglandin F-1 alpha sulfonamides: Potential treatments for osteoporosis

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.