Fullerene isoniazid conjugate--a tuberculostat with increased lipophilicity: synthesis and evaluation of antimycobacterial activity.

A fullerene-isoniazid conjugate has been synthesized by 1, 3 dipolar cycloaddition reaction of fullerene (C(60)) with isonicotinic acid (4-formyl-benzylidene) hydrazide and N-methylglycine. The identity and purity of the compound was confirmed by elemental analysis, (1)H NMR, (13)C NMR and MALDI-TOF mass spectral analysis. Stable water suspension, in which the particles of the synthesized conjugate were made to aggregate in nanosize, was successfully tested for antimycobacterial activity against Mycobacterium avium and strains of Mycobacterium tuberculosis- H(37)Rv & H6/99 at concentration as low as 0.

Fullerene derivatized s-triazine analogues as antimicrobial agents.

A series of novel fullerene derivatives bearing s-triazine moiety have been synthesized by adopting 1,3 dipolar cycloaddition reaction of C(60) and azomethine ylides generated from the corresponding Schiff bases of 2,4,6 trisubstituted s-triazine. All the compounds synthesized were characterized by elemental analysis, FT-IR, (1)H NMR, (13)C NMR and FAB-MS. The compounds were then screened for their antibacterial activity against both gram-positive (Staphylococcus aureus, Bacillus subtilis, Bacillus pumilis) and gram-negative (Escherichia coli, Pseudomonas aeruginosa and Klebsiella pneumoniae) bacteria by disc diffusion method.