[吡啶并(3,2 - e)(1,4)二氮杂䓬类——抗HIV - 1活性的合成与测试]
[Pyrido(3,2-e)(1,4)diazepines--synthesis and testing of anti-HIV-1 activity].
作者信息
Görlitzer K, Wilpert C, Rübsamen-Waigmann H, Suhartono H, Wang L, Immelmann A
机构信息
Institut für Pharmazeutische Chemie, Technischen Universität Braunschweig.
出版信息
Arch Pharm (Weinheim). 1995 Mar;328(3):247-55. doi: 10.1002/ardp.19953280308.
Starting from the commercially available 6-methyl-2-pyridylamine (1) the pyrido[3,2-e][1,4]diazepine 14a was synthesized in 12 steps with 7% total yield. 14a, the N-methyl derivative 14b, the thiolactam 15a, the amidine 16, and the 1,2,4-triazole 17 were tested for anti-HIV-1-activity. None of the compounds tested possesses antiviral activity comparable to that of zidovudine (3'-azido-3'-desoxythymidine = AZT).
从市售的6-甲基-2-吡啶胺（1）开始，经过12步反应合成了吡啶并[3,2-e][1,4]二氮杂卓14a，总产率为7%。对14a、N-甲基衍生物14b、硫代内酰胺15a、脒16和1,2,4-三唑17进行了抗HIV-1活性测试。所测试的化合物均不具有与齐多夫定（3'-叠氮基-3'-脱氧胸苷=AZT）相当的抗病毒活性。
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