Synthesis of Variously Substituted 1,8-Naphthyridine Derivatives and Evaluation of Their Antimycobacterial Activity

A series of 1,8-naphthyridine derivatives variously substituted in the 2, 3, 4 and 7 positions were synthesized for in vitro evaluation of antimycobacterial activity in accordance with an international program with the tuberculosis antimicrobial acquisition and coordinating facility (TAACF). Several compounds 4, 8, 12, 14, 19, 29 and 30, when tested at a concentration of 6.25 μg/ml against Mycobacterium tuberculosis H37Rv, showed an interesting activity with % inhibition in the range 38–96%. The most effective substituent in position 2, 4 or 7 of the 1,8-naphthyridine nucleus seem to be the piperidinyl group.