The Synthesis and Human FP Receptor Binding Affinity of 13,14-Dihydro Prostaglandin F_<1α> Sulfonamides : Potential Treatments for Osteoporosis

概要

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A novel class of saturated prostaglandin F_<2α> 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 nodified at the C_1 carboxylic acid moiety and at the C_<16>-C_<20> region of the prostaglandin. Based on the structure-activity relationships, it was found 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 was observed. These results are discussed within the framework of a proposed model for the human FP receptor.
公益社団法人日本薬学会の論文
2000-09-01