Cuadro A, Perez-Butragueño J, Pastor-Maeso M, Alvarez-Builla J, Martinez-Grueiro M M, Martinez-Fernandez A R
Departamento de Quimica Organica, Universidad de Alcala, Alcala de Henares, Spain.
Farmaco. 1992 Apr;47(4):477-88.
New 2-benzylideneimino- and 2-styryl-1,3-benzimidazole and benzothiazole derivatives have been prepared and tested in vitro against Caenorhabditis elegans, and Heligmosomoides polygyrus, showing some of them, interesting properties as inhibitors, which were not observed in the complementary in vivo tests. In order to rationalize the activity, log P was measured for all compounds, and QSAR models were developed, allowing the optimisation of the in vitro activity.
新型2-亚苄基亚氨基-和2-苯乙烯基-1,3-苯并咪唑及苯并噻唑衍生物已被制备，并针对秀丽隐杆线虫和多形螺旋线虫进行了体外测试，结果显示其中一些衍生物具有作为抑制剂的有趣特性，而在互补的体内测试中未观察到这些特性。为了阐明活性机制，测定了所有化合物的脂水分配系数（log P），并建立了定量构效关系（QSAR）模型，以优化体外活性。
