Pyridazino[3,4-b][1,5]Benzoxazepin-5(6H)-ones: Synthesis and Biological Evaluation

Author:

Barth B.1,Dierich M.2,Heinisch G.1,Jenny V.1,Matuszczak B.1,Mereiter K.3,Planer R.1,Schöpf I.1,Stoiber H.2,Traugott T.1,Aufschnaiter P. v.1

Affiliation:

1. Institute of Pharmaceutical Chemistry, University of Innsbruck, Innrain 52a, A-6020 Innsbruck, Austria

2. Institute of Hygiene/Ludwig-Boltzmann Institute for AIDS-Research, University of Innsbruck, Fritz-Pregl-Strasse 3, A-6020 Innsbruck, Austria

3. Institute of Mineralogy, Crystallography and Structural Chemistry, Technical University of Vienna, Getreidemarkt 9, A-1060 Vienna, Austria

Abstract

Starting from 3,6-dichloro-4-pyridazinecarboxylic acid chloride a series of novel pyridazino[3,4- b][1,5]benzoxazepin-5(6 H)-ones as 1,2-diazine isosters of nonnucleoside reverse transcriptase inhibitors was prepared via N-(2-hydroxyphenyl)-3,6-dichloro-4-pyridazinecarboxamides. The inhibition of HIV-1 reverse transcriptase was evaluated.

Publisher

SAGE Publications

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