二苯吡拉林衍生物的抗分枝杆菌活性。
Antimycobacterial activity of diphenylpyraline derivatives.
作者信息
Weis Robert, Faist Johanna, di Vora Ulrike, Schweiger Klaus, Brandner Barbara, Kungl Andreas J, Seebacher Werner
机构信息
Institute of Pharmaceutical Sciences, Pharmaceutical Chemistry, Karl-Franzens-University, Universitätsplatz 1, A-8010 Graz, Austria.
出版信息
Eur J Med Chem. 2008 Apr;43(4):872-9. doi: 10.1016/j.ejmech.2007.06.012. Epub 2007 Jul 10.
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.
二苯拉林的2-取代衍生物及其1-苯基和1-苯乙基类似物已通过几个步骤由二氢吡啶-2(1H)-硫酮制备而成。所有新化合物的结构均已通过核磁共振光谱法得到证实。它们对结核分枝杆菌H(37)Rv的活性以及对人细胞（HEK-293）的细胞毒性已通过体外试验测定。一般来说，在环的2位进行取代会提高抗分枝杆菌效力。最有前景的修饰是2-异丙基衍生物和1,2-二苯基类似物。
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