Synthesis of pyridazino[3,4-b][1,5]benzodiazepin-5-ones and their biological evaluation as non-nucleoside HIV reverse transcriptase inhibitors

被引：16
|
作者：
Heinisch, G
Huber, E
Matuszczak, B
Maurer, A
Prillinger, U
机构：
[1] Inst. of Pharmaceutical Chemistry, University of Innsbruck, Innrain 52a
来源：
ARCHIV DER PHARMAZIE | 1997年 / 330卷 / 1-2期
关键词：
HIV-1 reverse transcriptase inhibition; pyridazino[3,4-b][1,5]benzodiazepin-5-ones; non-nucleoside reverse transcriptase inhibitors;
D O I：
10.1002/ardp.19973300108
中图分类号：
R914 [药物化学];
学科分类号：
100701 ;
摘要：
Starting from 3,6-dichloro-N-(2-chIoro-5-nitrophenyl)-pyridazine-4-carboxamide (7) a series of 6,11-dialkylated pyridazino-[3,4-b][1,5]benzodiazepin-5-ones with a 3-chloro-8-nitro, 8-amino, 8-acetylamino, or 8-chloro substitution pattern was prepared via N-alkyl-3-alkylamino-6-chloro-N-(2-chloro-5-nitrophenyl)-pyridazine-4-carboxamides. The new compounds were screened as non-nucleoside reverse transcriptase inhibitors. The influence of the substitution pattern in compounds 10-13 on inhibitory potency is discussed.
引用
收藏
页码：29 / 34
页数：6
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