1-异烟酰基-4-芳酰基氨基硫脲化合物的研究

A STUDY OF 1-ISONICOTINOYL-4-AROYLTHIOSEMICARBAZIDES COMPOUNDS

进一步研究了卤代芳酰异硫氰与异烟酰肼反应,制得一系列1-异烟酰基-4-卤代芳酰基氨基硫脲,并观察了这些新药物的抗结核菌性能,其中以1-异烟酰基-4-对碘苯甲酰基-氨基硫脲抗结核菌作用最强。

For the purpose of studying the relation between molecular structure and tuberculostatic activity in acylthiosemicarbazide group,some new derivatives of thiosemicarbazide such as 1-isonicotinoyl-4-halogen-aroyl-thiosemicarbazides have been synthesized.These new compounds ware prepared by developing the reaction of the halogen aroylisothiocyanate with isonicotinoyl hydrazide In acetone,acetonitrile or djoxane in yield of 50-80%.Following is the reactionThe tuberculostatic activity of all the above compounds as compared with that of isonicotinoyl hydrazide have been measured.Inhibiting tuberculin test in vitro indicated that our compounds showed higher tuberculostatic activity than the corresponding 1-acyl-4-aryl-thiosemicar-bazides prepared by Buu-Hor and his co-workers.Among the compounds examined 1-isonicotinoyl-4-P-iodobenzoyl-thio-semicarbazide has been found to be the most active one(see table)for its minimum concentration of inhibition-10-8.