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抗结核药物研发:生物碱的影响。

Drug development against tuberculosis: Impact of alkaloids.

机构信息

Department of Chemistry, Institute of Science, Banaras Hindu University, Varanasi, 221005, Uttar Pradesh, India; Department of Pharmacology, Institute of Medical Sciences, Banaras Hindu University, Varanasi, 221005, Uttar Pradesh, India.

Department of Chemistry, Institute of Science, Banaras Hindu University, Varanasi, 221005, Uttar Pradesh, India.

出版信息

Eur J Med Chem. 2017 Sep 8;137:504-544. doi: 10.1016/j.ejmech.2017.06.005. Epub 2017 Jun 3.

Abstract

Despite of the advances made in the treatment and management, tuberculosis (TB) still remains one of main public health problem. The contrary effects of first and second-line anti-tuberculosis drugs have generated extended research interest in natural products in the hope of devising new antitubercular leads. Interestingly, plethoras of natural products have been discovered to exhibit activity towards various resistant strains of M. tuberculosis. Extensive applications of alkaloids in the field of therapeutics is well-established and nowday's researches being pursued to develop new potent drugs from natural sources for tuberculosis. Alkaloids are categorized in quite a few groups according to their structures and isolation from both terrestrial and marine sources. These new drugs might be a watershed in the battle against tuberculosis. This review summarizes alkaloids, which were found active against Mycobacteria since last ten years with special attention on the study of structure-activity relationship (SAR) and mode of action with their impact in drug discovery and development against tuberculosis.

摘要

尽管在治疗和管理方面取得了进展,但结核病(TB)仍然是主要的公共卫生问题之一。一线和二线抗结核药物的相反作用激发了人们对天然产物的广泛研究兴趣,希望设计出新的抗结核先导化合物。有趣的是,大量的天然产物已被发现对各种耐药结核分枝杆菌菌株具有活性。生物碱在治疗领域的广泛应用已经确立,现在的研究正在从天然来源中开发新的有效药物来治疗结核病。根据结构和从陆地及海洋来源的分离方法,生物碱可分为多个类别。这些新药可能是对抗结核病斗争的一个转折点。本文综述了近十年来发现的对分枝杆菌具有活性的生物碱,特别关注结构-活性关系(SAR)和作用方式的研究,以及它们在抗结核药物发现和开发中的影响。

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