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Bioorg Med Chem Lett. 2010 Nov 15;20(22):6538-41. doi: 10.1016/j.bmcl.2010.09.038. Epub 2010 Sep 16.
A new class of 2-substituted benzoxazole carboxamides are presented as potent functional 5-HT(3) receptor antagonists. The chemical series possesses nanomolar in vitro activity against human 5-HT(3)A receptors. A chemistry optimization program was conducted and identified 2-aminobenzoxazoles as orally active 5-HT(3) receptor antagonists with good metabolic stability. These novel analogues possess drug-like characteristics and have potential utility for the treatment of diseases attributable to improper 5-HT(3) receptor function, especially diarrhea predominant irritable bowel syndrome (IBS-D).
呈现出一类新型 2-取代苯并恶唑甲酰胺类化合物，它们作为强效功能性 5-HT(3)受体拮抗剂。该化学系列在体外对人 5-HT(3)A 受体具有纳摩尔级的活性。进行了化学优化程序，鉴定出 2-氨基苯并恶唑类化合物是具有口服活性的 5-HT(3)受体拮抗剂，具有良好的代谢稳定性。这些新型类似物具有类药性特征，对于治疗与 5-HT(3)受体功能不当相关的疾病具有潜在用途，特别是以腹泻为主的肠易激综合征（IBS-D）。
