The synthesis and human FP receptor binding affinity of 13,14-dihydro prostaglandia F1(α) sulfonamides: Potential treatments for osteoporosis

Article abstract of DOI:10.1248/cpb.48.1332

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 modified at the C₁ carboxylic acid moiety and at the C₁₆ - C₂₀ region of the prostaglandin. Based on the structure-activity relationships, it was found that at C₁, the aryl sulfonamide analogs possessed greater affinity for the hFP receptor when compared to alkyl sulfonamides. When the sulfonamide was introduced into the C₁₆ - C₂₀ 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.

Full text of DOI:10.1248/cpb.48.1332

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