Synthesis of some new 1,8-naphthyridine derivatives of expected biological activity

ABSTRACT

A series of some new 1,8-naphthyridine derivatives such as, 3-[2-thioxo-l,3,4-thiadiazolin-5-yl]-1,8-naphthyridines, 3-[2-substituted amino-1,3,4-thiadiazol-5-yl]-1,8-naphthyridines, 3-[6-substituted imidazo-[2,1-b]-l,3,4-thiadiazol-2-yl]-1,8-naphthyridines and other nitrogen, sulphur and/or oxygen heterocycles incorporated into 1,8-naphthyridine moities through an amide linkage has been synthesized for the purpose of biological evaluation. Compounds [2, 3, 5, 6, 8d, 10c, 11, 12, 14c] were tested for their antimicrobial activity against Gram +ve and Gram -ve bacteria and against a fungus [Aspergillus niger]. Among of these compounds only compounds 5 and 6 showed moderate activity against Aspergillus niger. Also, compounds 4a and 8c were tested against Ehrlich ascites carcinoma in mice and then measured for their cytotoxic activity against P388 Leukemia cells. Compounds 9b, 10b and 12 were tested against different types of turner cells in [USA]