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基于喹啉、香豆素及其他杂环类似物的HIV-1整合酶抑制剂

Quinoline, Coumarin and Other Heterocyclic Analogs Based HIV-1 Integrase Inhibitors.

作者信息

Wadhwa Pankaj, Jain Priti, Rudrawar Santosh, Jadhav Hemant R A

机构信息

Department of Pharmacy, Birla institute of Technology and Science Pilani, Pilani Campus, Pilani- 333031, Rajasthan, India.

Menzies Health Institute Queensland, Griffith University, Gold Coast 4222, Australia.

出版信息

Curr Drug Discov Technol. 2018;15(1):2-19. doi: 10.2174/1570163814666170531115452.

Abstract

Human Immunodeficiency Virus Type 1 Integrase or HIV-1 integrase (IN) is a 288 amino acid protein that incorporates the retrotranscribed viral DNA into the host chromosomal DNA. Over the past 30 years, large number of derivatives have been evaluated for their inhibitory potential against IN. There is vast literature available which need to be collated to help scientists plan the future drug design. This review discusses the reports of past 25 years on analogs of quinoline, coumarin and other related heterocycles, which exhibit low micromolar inhibitory potency against IN.

摘要

人类免疫缺陷病毒1型整合酶或HIV-1整合酶(IN)是一种由288个氨基酸组成的蛋白质,它将逆转录后的病毒DNA整合到宿主染色体DNA中。在过去30年里,大量衍生物已被评估其对IN的抑制潜力。有大量文献需要整理,以帮助科学家规划未来的药物设计。本综述讨论了过去25年中关于喹啉、香豆素及其他相关杂环类似物的报道,这些类似物对IN表现出低微摩尔抑制效力。

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