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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
Author(s) -
Heinisch Gottfried,
Huber Elisabeth,
Matuszczak Barbara,
Maurer Astrid,
Prillinger Ulrike
Publication year - 1997
Publication title -
archiv der pharmazie
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 0.468
H-Index - 61
eISSN - 1521-4184
pISSN - 0365-6233
DOI - 10.1002/ardp.19973300108
Subject(s) - chemistry , stereochemistry , nucleoside , pyridazine , reverse transcriptase , carboxamide , nitro , reverse transcriptase inhibitor , potency , chemical synthesis , ic50 , alkyl , in vitro , biochemistry , rna , organic chemistry , gene
Starting from 3,6‐dichloro‐ N ‐(2−chloro‐5‐nitrophenyl)‐pyrid‐azine‐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‐nitro‐phenyl)‐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.