Ertan M, Saygun N, Ureten M
Mikrobiyol Bul. 1985 Jul;19(3):121-6.
A new series of p-aminosalicylic acid derivatives were tested in vitro against Myc.tbc. H37Rv strain and clinically isolated pathogenic mycobacteria. 4 - [alpha - (benzylamino - thiocarbonylthio) - acetamido] - salicylic acid was most active, 4 - [alpha - methyl - alpha - (furfurylamino - thiocarbonylthio) - acetamido] - salicylic acid was more active than PAS. 4 - [alpha - (ethylamino - thiocarbonylthio) - acetamido] - salicylic acid, and 4 - [alpha - methyl - alpha - (ethylamino - thiocarbonylthio) - acetamido] - salicylic acid derivatives were nearly as active as PAS. The causes of increase in tuberculostatic activity can be assumed to be the isothiocyanate groups, which are the products of hydrolysis of the compounds investigated.
对一系列新的对氨基水杨酸衍生物进行了体外测试,以检测其对结核分枝杆菌H37Rv菌株和临床分离的致病性分枝杆菌的作用。4 - [α - (苄基氨基 - 硫代羰基硫基) - 乙酰胺基] - 水杨酸活性最强,4 - [α - 甲基 - α - (糠基氨基 - 硫代羰基硫基) - 乙酰胺基] - 水杨酸的活性高于对氨基水杨酸(PAS)。4 - [α - (乙氨基 - 硫代羰基硫基) - 乙酰胺基] - 水杨酸和4 - [α - 甲基 - α - (乙氨基 - 硫代羰基硫基) - 乙酰胺基] - 水杨酸衍生物的活性与PAS几乎相同。可以认为抑菌活性增加的原因是异硫氰酸酯基团,它们是所研究化合物的水解产物。