最近合成伐地考昔的方法：一种潜在的 3,4-二芳基异恶唑基 COX-II 抑制剂。
Recent methodologies toward the synthesis of valdecoxib: a potential 3,4-diarylisoxazolyl COX-II inhibitor.
机构信息
Torrey Pines Institute for Molecular Studies, Port St. Lucie, FL 34987, USA.
出版信息
Eur J Med Chem. 2010 Nov;45(11):4697-707. doi: 10.1016/j.ejmech.2010.07.045. Epub 2010 Aug 6.
Abstract
Non-steroidal anti-inflammatory drugs are widely used therapeutic agents in the treatment of inflammation, pain and fever. Cyclooxygenase catalyzes the initial step of biotransformation of arachidonic acid to prostanoids, and exist as three distinct isozymes; COX-I, COX-II and COX-III. Selective COX-II inhibitors are a class of potential anti-inflammatory, analgesic, and antipyretic drugs with reduced gastrointestinal (GI) side effects compared to nonselective inhibitors. 3,4-Diarylisoxazole scaffold is recurrently found in a wide variety of NSAIDs, protein kinase inhibitors, hypertensive agents, and estrogen receptor (ER) modulators. In the present review, we document on the recent synthetic strategies of 3,4-diarylisoxazolyl scaffolds of valdecoxib and its relevant structural analogues.
摘要
非甾体抗炎药是治疗炎症、疼痛和发热的广泛应用的治疗药物。环氧化酶催化花生四烯酸生物转化为前列腺素的初始步骤，存在三种不同的同工酶：COX-I、COX-II 和 COX-III。选择性 COX-II 抑制剂是一类具有潜在抗炎、镇痛和解热作用的药物，与非选择性抑制剂相比，胃肠道 (GI) 副作用减少。3,4-二芳基异恶唑骨架广泛存在于各种非甾体抗炎药、蛋白激酶抑制剂、抗高血压药和雌激素受体 (ER) 调节剂中。在本综述中，我们记录了伐地昔布及其相关结构类似物的 3,4-二芳基异恶唑基支架的最新合成策略。
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