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Pyridazines 82[1]. Synthesis of Pyridazino[3,4-b][1,5]benzodiazepin-5-ones and their Biological Evaluation as Non-nucleoside HIV Reverse Transcriptase Inhibitors

✍ Scribed by Gottfried Heinisch; Elisabeth Huber; Barbara Matuszczak; Astrid Maurer; Ulrike Prillinger

Publisher: John Wiley and Sons
Year: 1997
Tongue: English
Weight: 529 KB
Volume: 330
Category: Article
ISSN: 0365-6233
DOI: 10.1002/ardp.19973300108

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✦ Synopsis

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.

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