Sriram Dharmarajan, Bal Tanushree Ratan, Yogeeswari Perumal
Medicinal Chemistry Research Laboratory, Pharmacy Group, Birla Institute of Technology and Science, Pilani 333031, India.
J Pharm Pharm Sci. 2005 Oct 20;8(3):565-77.
HIV is the most significant risk factor for many opportunistic infections such as tuberculosis, hepatitis, bacterial infections and others. In this paper, we describe an aminopyrimidinimino isatin lead compound as a novel non-nucleoside reverse transcriptase inhibitor with broad-spectrum chemotherapeutic properties for the effective treatment of AIDS and AIDS-related opportunistic infections.
The synthesis of various aminopyrimidinimino isatin derivatives was achieved in two steps and evaluated for anti-HIV, anti-HCV, antimycobacterial and antibacterial activities.
Compound 1-cyclopropyl-6-fluoro-1,4-dihydro-4-oxo-7[[N4-[3'-(4'-amino-5'-trimethoxybenzylpyrimidin-2'-yl)imino-1'-isatinyl] methyl]N1-piperazinyl]-3-quinoline carboxylic acid (14) emerged as the most potent broad-spectrum chemotherapeutic agent active against HIV, HCV, M. tuberculosis and various pathogenic bacteria. Among the synthesized compounds compound 14 and 15 emerged as more promising broad-spectrum chemotherapeutic agents.
人类免疫缺陷病毒（HIV）是许多机会性感染（如结核病、肝炎、细菌感染等）的最重要风险因素。在本文中，我们描述了一种氨基嘧啶亚氨基异吲哚酮先导化合物，它是一种新型非核苷逆转录酶抑制剂，具有广谱化疗特性，可有效治疗艾滋病及与艾滋病相关的机会性感染。
通过两步法合成了各种氨基嘧啶亚氨基异吲哚酮衍生物，并对其抗HIV、抗丙型肝炎病毒（HCV）、抗分枝杆菌和抗菌活性进行了评估。
化合物1-环丙基-6-氟-1,4-二氢-4-氧代-7[[N4-[3'-(4'-氨基-5'-三甲氧基苄基嘧啶-2'-基)亚氨基-1'-异吲哚酮基]甲基]N1-哌嗪基]-3-喹啉羧酸（14）成为对HIV、HCV、结核分枝杆菌和各种病原菌最具活性的广谱化疗药物。在合成的化合物中，化合物14和15成为更有前景的广谱化疗药物。
