Synthesis and antitubercular activity of N-(2-naphthyl)glycine hydrazide analogues

Article abstract of DOI:10.1021/jm00131a002

N-(2-Naphthyl)glycine hydrazide analogues were synthesized and tested for possible in vitro antitubercular activity. N-(2-Naphthyl)alanine hydrazide, N-methyl-N-(2-naphthyl)glycine hydrazide, N-(6-methoxy-2-naphthyl)glycine hydrazide, and 3-(2-naphthylamino)butyric acid hydrazide showed potent inhibitory action against Mycobacterium tuberculosis H₃₇R(v) in Youman's medium at concentrations ranging from 0.5 to 10.0 μg/mL. These compounds showed significant inhibitory action against isonicotinic acid hydrazide and streptomycin-resistant strains of M. tuberculosis. N-(6-Quinolyl)glycine hydrazide and 3-(2-quinolylamino)butyric acid hydrazide, which are bioisosteres of compounds 1 and 23, showed loss of antitubercular activity at low concentrations.