新型2,5-二取代-1,3,4-噻二唑的合成及其抗惊厥和抗菌活性的初步评价。
Synthesis of new 2,5-disubstituted-1,3,4-thiadiazoles and preliminary evaluation of anticonvulsant and antimicrobial activities.
作者信息
Dogan Hatice N, Duran Arzu, Rollas Sevim, Sener Göksel, Uysal Meral K, Gülen Dumrul
机构信息
Department of Pharmaceutical Chemistry, Faculty of Pharmacy, Marmara University, 81010 Haydarpasa, Istanbul, Turkey.
出版信息
Bioorg Med Chem. 2002 Sep;10(9):2893-8. doi: 10.1016/s0968-0896(02)00143-8.
Two new series of 2,5-disubstituted-1,3,4-thiadiazoles were synthesized for their possible anticonvulsant, antibacterial and antifungal activities. The degree of protection afforded by these compounds at a dose of 100mg/kg i.p. against pentylenetetrazole-induced convulsions in mice ranged from 0 to 90%. Among these compounds, 2a (90%) and 2g (70%) showed maximum protection. Antimicrobial tests showed that the MIC value of 3j against Pseudomanas aeruginosa was equal to that of penicillin.
合成了两个新系列的2,5 - 二取代 - 1,3,4 - 噻二唑，以研究其可能的抗惊厥、抗菌和抗真菌活性。这些化合物以100mg/kg腹腔注射给药时，对小鼠戊四氮诱导惊厥的保护程度在0%至90%之间。在这些化合物中，2a（90%）和2g（70%）表现出最大的保护作用。抗菌测试表明，3j对铜绿假单胞菌的最低抑菌浓度值与青霉素相当。
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