Wang Y, Soper D L, Dirr M J, deLong M A, De B, Wos J A
Procter and Gamble Pharmaceuticals, Mason, OH 45040-8006, USA.
Chem Pharm Bull (Tokyo). 2000 Sep;48(9):1332-7. doi: 10.1248/cpb.48.1332.
A novel class of saturated prostaglandin F2alpha 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.
已合成了一类新型的饱和前列腺素F2α磺酰胺类似物,并在人FP受体结合试验中进行了评估,以确定其在治疗骨质疏松症方面的潜在用途。这些化合物在前列腺素的C1羧酸部分和C16 - C20区域进行了修饰。基于构效关系,发现与烷基磺酰胺相比,在C1处芳基磺酰胺类似物对hFP受体具有更高的亲和力。当将磺酰胺引入前列腺素的C16 - C20区域(ω链)时,观察到结合显著降低。在提出的人FP受体模型框架内讨论了这些结果。