Synthesis and local anaesthetic activities of 2-aminothiazole/thiadiazole analogues of lidocaine
作者:Naveen P. Badiger、Ashraf Khan、M. B. Kalashetti、I. M. Khazi
DOI:10.1007/s00044-011-9659-4
日期:2012.8
Various 2-aminothiazole and 2-aminothiadiazole derivatives viz N-[4-(2-Chloro-4-fluoro-phenyl)-thiazol-2-yl]-2-substituted acetamides (3a, 4a, 5a) and N-[5-(4-substituted aryl)-[1,3,4]thiadiazol-2-yl]-2-acetamides (3b, 3c, 4b, 4c, 5b, 5c) were synthesized from their corresponding properly substituted 2-aminothiazoles and 2-aminothiadiazoles. Structures of all the newly synthesized compounds were established by analytical and spectral data. Synthesized compounds were screened for their local anaesthetic activity using the rat sciatic nerve model.Various 2-aminothiazole and 2-aminothiadiazole derivatives viz N-[4-(2-Chloro-4-fluoro-phenyl)-thiazol-2-yl]-2-substituted acetamides (3a, 4a, 5a) and N-[5-(4-substituted aryl)-[1,3,4]thiadiazol-2-yl]-2-acetamides (3b, 3c, 4b, 4c, 5b, 5c) were synthesized from their corresponding properly substituted 2-aminothiazoles and 2-aminothiadiazoles. Structures of all the newly synthesized compounds were established by analytical and spectral data. Synthesized compounds were screened for their local anaesthetic activity using the rat sciatic nerve model.