Local anaesthetics. Part III. Local anaesthetic activity and synthesis of 2-(N-substituted or N,N-disubstituted aminoacetamido)-4-aryl thiazoles.
作者:Ram LAKHAN、Om Prakash SINGH
DOI:10.1271/bbb1961.48.1441
日期:——
Some new 2-(N-substituted or N, N-disubstituted aminoacetamido)-4-p-nitrophenyl, 4-m-nitrophenyl and 4-(2', 5'-dimethoxy)phenyl thiazoles were synthesised. Their hydrochlorides were screened for local anaesthetic activity by Frog's sciatic plexus method and this activity compared with that of procaine hydrochloride. Among them, the 2-(N-substituted aminoacetamido)-4-m-nitrophenylthiazole hydrochlorides are the most potent: almost twice in terms of the onset of anaesthesia in comparison with procaine-HCl.
一些新的2-(N取代或N,N双取代氨基乙酰氨基)-4-对硝基苯、4-邻硝基苯和4-(2',5'-二甲氧基)苯噻唑被合成。它们的盐酸盐通过青蛙坐骨神经丛法筛选局部麻醉活性,并与盐酸普鲁卡因的活性进行了比较。其中,2-(N取代氨基乙酰氨基)-4-邻硝基苯噻唑盐酸盐的活性最强:在麻醉起效时间上几乎是盐酸普鲁卡因的两倍。