Heinisch G, Huber E, Matuszczak B, Maurer A, Prillinger U
Institute of Pharmaceutical Chemistry, University of Innsbruck, Austria.
Arch Pharm (Weinheim). 1997 Jan-Feb;330(1-2):29-34. doi: 10.1002/ardp.19973300108.
Starting from 3,6-dichloro-N-(2-chloro-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.
从3,6-二氯-N-(2-氯-5-硝基苯基)-哒嗪-4-甲酰胺(7)出发，通过N-烷基-3-烷基氨基-6-氯-N-(2-氯-5-硝基苯基)-哒嗪-4-甲酰胺制备了一系列具有3-氯-8-硝基、8-氨基、8-乙酰氨基或8-氯取代模式的6,11-二烷基哒嗪并[3,4-b][1,5]苯并二氮杂卓-5-酮。这些新化合物作为非核苷类逆转录酶抑制剂进行了筛选。讨论了化合物10-13中取代模式对抑制活性的影响。
