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杂环化合物作为碳酸酐酶抑制剂。

Heterocyclic compounds as carbonic anhydrase inhibitor.

机构信息

Department of Pharmaceutical Chemistry, Faculty of Pharmacy, Jamia Hamdard (Hamdard University), Hamdard Nagar, New Delhi, India.

出版信息

J Enzyme Inhib Med Chem. 2012 Dec;27(6):773-83. doi: 10.3109/14756366.2011.617882. Epub 2011 Oct 10.

Abstract

The carbonic anhydrases (CAs, EC 4.2.1.1) constitute interesting targets for the design of pharmacological agents useful in the treatment or prevention of a variety of disorders such as, glaucoma, acid-base disequilibria, epilepsy, and other neuromuscular diseases, altitude sickness, edema, and obesity. A quite new and unexpected application of the CA inhibitors (CAIs) is with regard to their potential use in the management (imaging and treatment) of hypoxic tumors. A series of sulfonamides, including some clinically used derivatives like acetazolamide, methazolamide, ethoxzolamide, dichlorophenamide, dorzolamide, brinzolamide, benzolamide, and sulpiride, or indisulam, a compound in clinical development as antitumor drug, as well as the sulfamate antiepileptic drug topiramate have been reported to inhibit various human carbonic anhydrase isozyme. Various heterocyclic sulfonamides have been reported in this review with their potency to inhibit different carbonic anhydrases isozymes.

摘要

碳酸酐酶(CAs,EC 4.2.1.1)是设计用于治疗或预防多种疾病的药理学药物的有趣靶点,如青光眼、酸碱失衡、癫痫和其他神经肌肉疾病、高原病、水肿和肥胖症。碳酸酐酶抑制剂(CAIs)的一个相当新的和意外的应用是关于它们在缺氧肿瘤的管理(成像和治疗)中的潜在用途。一系列磺酰胺类药物,包括一些临床使用的衍生物,如乙酰唑胺、甲唑胺、依索唑胺、二氯苯酰胺、多佐胺、布林佐胺、苯佐胺和舒必利,或正在临床开发作为抗肿瘤药物的 indisulam,以及磺胺类抗癫痫药物托吡酯,已被报道可抑制各种人碳酸酐酶同工酶。本文综述了各种杂环磺酰胺类化合物,它们具有抑制不同碳酸酐酶同工酶的活性。

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