Sanna Paolo, Carta Antonio, Gherardini Laura, Esmail Mohammad, Nikookar Rahbar
Dipartimento Farmaco-Chimico-Tossicologico, Università degli Studi, Sassari, Italy.
Farmaco. 2002 Jan;57(1):79-87. doi: 10.1016/s0014-827x(01)01174-0.
A series of 32 3-aryl-, 3-cyclohexyl-, and 3-heteroaryl-substituted-2-(1H(2H)-benzotriazol-1(2)-yl)-prop-2-enenitriles, prop-2-enamides and propenoic acids, was synthesized as a part of our research in the antitubercular field, according to an international program with the Tuberculosis Antimicrobial Acquisition and Coordinating Facility (TAACF). This work reports the preparation and analytical and spectroscopic characterization (MS, UV, IR, 1H NMR) of all compounds synthesized. Among these only a few compounds (E-4b,c, E-5a, E-7e and E-8d) were found to be endowed with modest growth inhibition of Mycobacterium tuberculosis. However, the obtained results allowed to acquire interesting structure-activity relationships.
作为我们抗结核领域研究的一部分，根据与结核病抗菌药物采购与协调机构（TAACF）的国际项目，合成了一系列32种3-芳基、3-环己基和3-杂芳基取代的2-(1H(2H)-苯并三唑-1(2)-基)-丙-2-烯腈、丙-2-烯酰胺和丙酸。这项工作报道了所有合成化合物的制备以及分析和光谱表征（质谱、紫外光谱、红外光谱、氢核磁共振谱）。其中仅发现少数化合物（E-4b、c，E-5a，E-7e和E-8d）对结核分枝杆菌具有适度的生长抑制作用。然而，所获得的结果有助于得出有趣的构效关系。
