Kumar Suresh, Ali Md Rahmat, Bawa Sandhya
Department of Pharmaceutical Chemistry, Faculty of Pharmacy, Jamia Hamdard, New Delhi, India.
J Pharm Bioallied Sci. 2014 Oct;6(4):222-8. doi: 10.4103/0975-7406.142943.
Trypanosomiasis and leishmaniasis are two most ruinous parasitic infectious diseases caused by Trypanosoma and Leishmania species. The disease affects millions of people all over the world and associated with high morbidity and mortality rates. The review discuss briefly on current treatment of these parasitic diseases and trypanothione reductase (TryR) as potential targets for rational drug design. The enzyme trypanothione reductase (TryR) has been identified as unique among these parasites and has been proposed to be an effective target against for developing new drugs. The researchers have selected this enzyme as target is due to its substrate specificity in contrast to human analogous glutathione reductase and its absence from the host cell which makes this enzyme an ideal target for drug discovery. In this review we have tried to present an overview of the different tricyclic compounds which are potent inhibitors of TryR with their inhibitory activities against the parasites are briefly discussed.
锥虫病和利什曼病是由锥虫属和利什曼原虫属引起的两种最具毁灭性的寄生虫传染病。该疾病影响着全球数百万人，且发病率和死亡率很高。本综述简要讨论了这些寄生虫疾病的当前治疗方法以及作为合理药物设计潜在靶点的锥虫硫醇还原酶（TryR）。锥虫硫醇还原酶（TryR）已被确定为这些寄生虫中独特的一种，并被提议作为开发新药的有效靶点。研究人员选择该酶作为靶点是因为其底物特异性与人类类似的谷胱甘肽还原酶不同，且宿主细胞中不存在该酶，这使得该酶成为药物发现的理想靶点。在本综述中，我们试图概述不同的三环化合物，这些化合物是TryR的有效抑制剂，并简要讨论了它们对寄生虫的抑制活性。
