Sriram D, Yogeeswari P, Meena K
Medicinal Chemistry Research Laboratory, Pharmacy Group, Birla Institute of Technology and Science, Pilani 333031, India.
Pharmazie. 2006 Apr;61(4):274-7. doi: 10.1002/chin.200629154.
HIV is the most significant risk factor for many opportunistic infections like tuberculosis. In this study, we designed an isatinimino lead compound as a novel non-nucleoside reverse transcriptase inhibitor with antimycobacterial properties for the effective treatment of AIDS and AIDS-related tuberculosis. Among the compounds sythesized, 1-cyclopropyl-6-fluoro-8-methoxy-1,4-dihydro-4-oxo-7[[N4-[3'-[(4,6-dimethylpyrimidin-2-yl)benzenesulfonamido-4-yl]imino-1'-(5-fluoroisatinyl)]methyl]-3-methyl N1-piperazinyl]-3-quinoline carboxylic acid (9) emerged as the most potent broad-spectrum chemotherapeutic agent active against HIV (EC50: 12.1 microg/ml), and Mycobacterium tuberculosis (MIC: 1.22 microg/ml).
人类免疫缺陷病毒（HIV）是许多机会性感染（如结核病）的最重要风险因素。在本研究中，我们设计了一种异吲哚酮亚胺先导化合物，作为一种具有抗分枝杆菌特性的新型非核苷逆转录酶抑制剂，用于有效治疗艾滋病及艾滋病相关结核病。在所合成的化合物中，1-环丙基-6-氟-8-甲氧基-1,4-二氢-4-氧代-7[[N4-[3'-[(4,6-二甲基嘧啶-2-基)苯磺酰胺基-4-基]亚氨基-1'-(5-氟异吲哚酮基)]甲基]-3-甲基-N1-哌嗪基]-3-喹啉羧酸（9）成为对HIV（半数有效浓度：12.1微克/毫升）和结核分枝杆菌（最低抑菌浓度：1.22微克/毫升）具有活性的最有效的广谱化疗药物。
