Antimycobacterial activity of diphenylpyraline derivatives

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• 作者：Robert Weis ; Johanna Faist ; Ulrike di Vora ; Klaus Schweiger ; Barbara Br ; ner ; Andreas J. Kungl ; Werner Seebacher
• 关键词：4-Alkoxypiperidine ; Antimycobacterial activity ; In vitro assay ; Piperidin-4-ol ; Synthesis
• 刊名：European Journal of Medicinal Chemistry
• 出版年：2008
• 出版时间：April 2008
• 年：2008
• 卷：43
• 期：4
• 页码：872-879
• 全文大小：247 K

文摘

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 H₃₇Rv 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.