Departamento de Antibióticos, Universidade Federal de Pernambuco, Recife 50670-901, Brazil.
Eur J Med Chem. 2010 Sep;45(9):3685-91. doi: 10.1016/j.ejmech.2010.05.017. Epub 2010 May 31.
In this work we reported the synthesis and evaluation of anti-Toxoplasma gondii and antimicrobial activities in vitro of three new compound series obtained from ethyl(5-methyl-1-H-imidazole-4-carboxylate): acylthiosemicarbazide analogues 3a-d, 4-thiazolidinone analogues 4a-d and 1,3,4-thiadiazole analogues 5a-d. All synthesized compounds were characterized by IR, (1)H, (13)C NMR and HRMS. The majority of the tested compounds show excellent anti-T. gondii activity when compared to hydroxyurea and sulfadiazine. In addition it was also shown that most of the compounds in this study have a better performance against intracellular tachyzoites. The results for antimicrobial activity evaluation showed weak antibacterial and antifungal activities for all the tested molecules, when compared with the standard drugs (chloramphenicol and rifampicin for antibacterial activity; nistatin and ketoconazole for antifungal activity).
在这项工作中,我们报道了三种新的化合物系列的合成和体外抗弓形虫和抗菌活性评估,这些化合物是从乙基(5-甲基-1-H-咪唑-4-羧酸酯):酰基硫代半卡巴腙类似物 3a-d、4-噻唑烷酮类似物 4a-d 和 1,3,4-噻二唑类似物 5a-d 得到的。所有合成的化合物均通过 IR、(1)H、(13)C NMR 和 HRMS 进行了表征。与羟脲和磺胺嘧啶相比,大多数测试化合物表现出优异的抗弓形虫活性。此外,研究还表明,本研究中的大多数化合物对细胞内速殖子的效果更好。抗菌活性评估的结果表明,与标准药物(用于抗菌活性的氯霉素和利福平;用于抗真菌活性的制霉菌素和酮康唑)相比,所有测试分子的抗菌和抗真菌活性都较弱。