Chapleo C B, Myers P L, Smith A C, Stillings M R, Tulloch I F, Walter D S
Department of Medicinal Chemistry, Reckitt and Colman plc, Kingston-upon-Hull, United Kingdom.
J Med Chem. 1988 Jan;31(1):7-11. doi: 10.1021/jm00396a004.
Two different structural types of 2-aryl-1,3,4-thiadiazole amidines were synthesized and evaluated for anticonvulsant activity. Enhancement of the inherent anticonvulsant activity therein and separation of this activity from the accompanying sedative action of these compounds were attempted. The most potent compounds occurred in the 2-(trifluoromethyl)phenyl series of type 3 amidines, but they also possessed a relatively high level of neurotoxicity and sedation as demonstrated in the rotorod test.
合成了两种不同结构类型的2-芳基-1,3,4-噻二唑脒，并对其抗惊厥活性进行了评估。试图增强其中固有的抗惊厥活性，并将这种活性与这些化合物伴随的镇静作用区分开来。最有效的化合物出现在3型脒的2-(三氟甲基)苯基系列中，但如在转棒试验中所示，它们也具有相对较高水平的神经毒性和镇静作用。
