首页> 外文期刊>European Journal of Medicinal Chemistry: Chimie Therapeutique >Recent methodologies toward the synthesis of valdecoxib: a potential 3,4-diarylisoxazolyl COX-II inhibitor.
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Recent methodologies toward the synthesis of valdecoxib: a potential 3,4-diarylisoxazolyl COX-II inhibitor.

机译:伐地考昔合成的最新方法:潜在的3,4-二芳基异恶唑基COX-II抑制剂。

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摘要

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.
机译:非甾体抗炎药被广泛用于治疗炎症,疼痛和发烧。环氧合酶催化花生四烯酸生物转化为类前列腺素的起始步骤,并以三种不同的同工酶形式存在。 COX-I,COX-II和COX-III。选择性COX-II抑制剂是一类潜在的消炎,镇痛和解热药,与非选择性抑制剂相比,具有降低的胃肠道(GI)副作用。在各种NSAID,蛋白激酶抑制剂,高血压药和雌激素受体(ER)调节剂中经常发现3,4-二芳基异恶唑支架。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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