Pharmaceutical Research Center, Asahi Kasei Pharma Corporation, 632-1 Mifuku, Izunokuni-shi, Shizuoka 410-2321, Japan.
Bioorg Med Chem Lett. 2013 Dec 15;23(24):6569-76. doi: 10.1016/j.bmcl.2013.10.065. Epub 2013 Nov 6.
We describe a medicinal chemistry approach for generating a series of 2-(1H-pyrazol-1-yl)thiazoles as EP1 receptor antagonists. To improve the physicochemical properties of compound 1, we investigated its structure-activity relationships (SAR). Optimization of this lead compound provided small compound 25 which exhibited the best EP1 receptor antagonist activity and a good SAR profile.
我们描述了一种药物化学方法，用于生成一系列 2-(1H-吡唑-1-基)噻唑作为 EP1 受体拮抗剂。为了改善化合物 1 的物理化学性质，我们研究了其构效关系（SAR）。对该先导化合物进行优化得到了小分子化合物 25，其表现出最佳的 EP1 受体拮抗剂活性和良好的 SAR 特征。
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