Camoutsis Charalabos, Geronikaki Athina, Ciric Ana, Soković Marina, Zoumpoulakis Panagiotis, Zervou Maria
School of Health Sciences, Department of Pharmacy, Laboratory of Pharmaceutical Chemistry, University of Patras, Patras 26500, Greece.
Chem Pharm Bull (Tokyo). 2010 Feb;58(2):160-7. doi: 10.1248/cpb.58.160.
A series of thirteen new thiadiazole compounds were synthesized and evaluated for in vitro antifungal and antibacterial activity. All compound tested showed significant antifungal activity against all the micromycetes, compared to the commercial fungicide bifonazole. Differences in their activity depend on the substitution of different reactive groups. More specifically, best antifungal activity was shown for the synthetic analogue with methylpiperazine reactive group. Furthermore, it is apparent that different compounds reacted on different ways against bacteria. An effort was made to correlate the above mentioned differences in activity with lipophilicity studies. Furthermore, NMR and molecular modelling were used to obtain the main conformational features of a potent analogue, for future in silico studies.
合成了一系列13种新型噻二唑化合物，并对其体外抗真菌和抗菌活性进行了评估。与市售杀真菌剂联苯苄唑相比，所有测试化合物对所有微真菌均表现出显著的抗真菌活性。它们的活性差异取决于不同反应基团的取代情况。更具体地说，具有甲基哌嗪反应基团的合成类似物表现出最佳的抗真菌活性。此外，很明显不同化合物对细菌的反应方式不同。已努力将上述活性差异与亲脂性研究相关联。此外，利用核磁共振（NMR）和分子建模来获得一种有效类似物的主要构象特征，以供未来的计算机模拟研究使用。
