European Journal of Medicinal Chemistry 2008-04-01

Antimycobacterial activity of diphenylpyraline derivatives.

Robert Weis, Johanna Faist, Ulrike di Vora, Klaus Schweiger, Barbara Brandner, Andreas J Kungl, Werner Seebacher

Index: Eur. J. Med. Chem. 43 , 872-9, (2008)

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Abstract

2-Substituted derivatives of diphenylpyraline and their 1-phenyl and 1-phenethyl analogues have been prepared in several steps from dihydropyridine-2(1H)-thiones. The structures of all new compounds have been confirmed by NMR spectroscopy. Their activity against Mycobacterium tuberculosis H(37)Rv as well as their cytotoxicity against human cells (HEK-293) have been determined via in vitro assays. The antimycobacterial potency was in general increased by substitution in ring position 2. The most promising modifications were a 2-isopropyl derivative and a 1,2-diphenyl analogue.