Newer aminopyrimidinimino isatin analogues as non-nucleoside HIV-1 reverse transcriptase inhibitors for HIV and other opportunistic infections of AIDS: design, synthesis and biological evaluation

D. Sriram, T.R. Bal, P. Yogeeswari
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Abstract

Human immuno deficiency virus (HIV) weakens the immune system so that many opportunistic infections (OIs) like tuberculosis, hepatitis, bacterial infections etc can develop. In this paper, we designed aminopyrimidinimino isatin lead compound as a novel non-nucleoside reverse transcriptase inhibitor (NNRTI) with broad-spectrum chemotherapeutic properties for the effective treatment of AIDS and AIDS-related OIs. Compound 1-cyclopropyl-6-fluoro-1,4-dihydro-4-oxo-7-[[N4-[3'-(4'-amino-5'-trimethoxybenzyl pyrimidin-2'-yl)imino-1'-(5-methylisatinyl)]methyl]-N1-piperazinyl]-3-quinoline carboxylic acid (10) emerged as the most potent broad-spectrum chemotherapeutic agent active against HIV, HCV, Mycobacterium tuberculosis and various pathogenic bacteria.

新型氨嘧啶酰亚胺类似物作为HIV-1非核苷类逆转录酶抑制剂用于HIV和其他艾滋病机会性感染:设计、合成和生物学评价
人类免疫缺陷病毒(HIV)会削弱免疫系统,从而导致许多机会性感染(oi),如结核病、肝炎、细菌感染等。在本文中,我们设计了一种新型的非核苷类逆转录酶抑制剂(NNRTI),具有广谱化疗特性,可有效治疗艾滋病和艾滋病相关的oi。化合物1-环丙基-6-氟-1,4-二氢-4-氧-7-[[N4-[3'-(4'-氨基-5'-三甲氧基苄基嘧啶-2'-基)亚胺-1'-(5-甲基化atinyl)]甲基]- n1 -哌嗪基]-3-喹啉羧酸(10)是目前最有效的抗HIV、HCV、结核分枝杆菌和各种致病菌的广谱化疗药物。
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