Mavrova Anelia Ts, Anichina Kamelya K, Vuchev Dimitar I, Tsenov Jordan A, Kondeva Magdalena S, Micheva Mitka K
University of Chemical Technology and Metallurgy, 8 Kliment Ohridski Boulevard, 1756 Sofia, Bulgaria.
Bioorg Med Chem. 2005 Oct 1;13(19):5550-9. doi: 10.1016/j.bmc.2005.06.046.
Some new thiazolo[3,2-a]benzimidazolone derivatives were synthesized using two methods. The structures of the synthesized compounds were proved by means of IR, (1)H NMR and mass spectral data. Ab initio computations were performed in order to determine the electronic structure and geometry of the investigated molecules and to compare it to the geometry of albendazole. Biologically, experiments in vitro and in vivo were accomplished in order to identify the efficacy of the obtained thiazolobenzimidazolones against Trichinella spiralis. The effectiveness of compounds 4a-c in the intestinal phase of trichinellosis was 100% and in the muscle phase were 88% and 80% at a concentration of 100mg/kg mw for the compounds 4a and 4c. The results of the hepatotoxicity test showed that the compounds 4a and 4b possess hepatotoxicity comparable to that of albendazole.
使用两种方法合成了一些新的噻唑并[3,2 - a]苯并咪唑酮衍生物。通过红外光谱、¹H核磁共振和质谱数据证实了合成化合物的结构。进行了从头算计算，以确定所研究分子的电子结构和几何结构，并将其与阿苯达唑的几何结构进行比较。在生物学方面，进行了体外和体内实验，以确定所得噻唑并苯并咪唑酮对旋毛虫的疗效。化合物4a - c在旋毛虫病肠道阶段的有效性为100%，在肌肉阶段，化合物4a和4c在浓度为100mg/kg体重时的有效性分别为88%和80%。肝毒性测试结果表明，化合物4a和4b具有与阿苯达唑相当的肝毒性。
