SYNTHESIS OF PYRIDAZINO[3,4-B][1,5]BENZODIAZEPIN-5-ONES AND THEIR BIOLOGICAL EVALUATION AS NONNUCLEOSIDE HIV REVERSE-TRANSCRIPTASE INHIBITORS

Authors
HEINISCH G HUBER E MATUSZCZAK B MAURER A PRILLINGER U
Citation
G. Heinisch et al., SYNTHESIS OF PYRIDAZINO[3,4-B][1,5]BENZODIAZEPIN-5-ONES AND THEIR BIOLOGICAL EVALUATION AS NONNUCLEOSIDE HIV REVERSE-TRANSCRIPTASE INHIBITORS, Archiv der pharmazie, 330(1-2), 1997, pp. 29-34
Citations number
25
Categorie Soggetti
Chemistry,"Pharmacology & Pharmacy
Journal title
Archiv der pharmazie → ACNP
ISSN journal
03656233
Volume
330
Issue
1-2
Year of publication
1997
Pages
29 - 34
Database
ISI
SICI code
0365-6233(1997)330:1-2<29:SOPATB>2.0.ZU;2-M
Abstract
Starting from -(2-chIoro-5-nitrophenyl)-pyridazine-4-carboxamide (7) a series of 6,11-dialkylated pyridazino-[3,4-b][1,5]benzodiazepin-5-one s with a 3-chloro-8-nitro, 8-amino, 8-acetylamino, or 8-chloro substit ution pattern was prepared via 2-chloro-5-nitrophenyl)-pyridazine-4-ca rboxamides. 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.