Gülerman N, Rollas S, Kiraz M, Ekinci A C, Vidin A
Department of Pharmaceutical Chemistry, Faculty of Pharmacy, Marmara University, Istanbul, Turkey.
Farmaco. 1997 Nov;52(11):691-5.
Some new 1-(4-fluorobenzoyl)-4-alkyl/arylthiosemicarbazide (2a-g), 5-(4-fluorophenyl)4-alkyl/aryl-2,4-dihydr-3H-1,2,4-triazole-3-thio ne (3a-g) derivatives, 3-(benzylthio)-5-(4-fluorophenyl)-4-phenyl-4H-1,2,4-triazole (3h) and 2-acetyl-5-(4-fluorophenyl)-4-phenyl-2,4-dihydro-3H-1,2,4-triazole-3-thi one (3i) were prepared and tested for their antimycobacterial and anticonvulsant activities. The structure of compounds was confirmed by elemental analyses and spectroscopic techniques. The antimycobacterial activity of the synthesized compounds was investigated against M. fortiutum ATCC 6841 and most of them were found active against the above strain with MIC values of 64 or 32 micrograms/ml. The anticonvulsant activity of the 2d, 3d-i was determined against pentylenetetrazole induced seizures. 3f-i showed anticonvulsant activity (10 to 30% protection).
制备了一些新型的1-(4-氟苯甲酰基)-4-烷基/芳基硫代氨基脲(2a-g)、5-(4-氟苯基)-4-烷基/芳基-2,4-二氢-3H-1,2,4-三唑-3-硫酮(3a-g)衍生物、3-(苄硫基)-5-(4-氟苯基)-4-苯基-4H-1,2,4-三唑(3h)和2-乙酰基-5-(4-氟苯基)-4-苯基-2,4-二氢-3H-1,2,4-三唑-3-硫酮(3i)，并对其抗分枝杆菌和抗惊厥活性进行了测试。通过元素分析和光谱技术确定了化合物的结构。研究了合成化合物对偶然分枝杆菌ATCC 6841的抗分枝杆菌活性，发现它们中的大多数对上述菌株具有活性，最低抑菌浓度值为64或32微克/毫升。测定了2d、3d-i对戊四氮诱导惊厥的抗惊厥活性。3f-i显示出抗惊厥活性(10%至30%的保护作用)。
