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Fullerene Isoniazid Conjugate – A Tuberculostat with Increased Lipophilicity: Synthesis and Evaluation of Antimycobacterial Activity
Author(s) -
Kumar Anish,
Patel Gaurang,
Me Shobhana Karuveettil
Publication year - 2009
Publication title -
chemical biology and drug design
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 0.59
H-Index - 77
eISSN - 1747-0285
pISSN - 1747-0277
DOI - 10.1111/j.1747-0285.2009.00804.x
Subject(s) - antimycobacterial , conjugate , hydrazide , lipophilicity , isoniazid , chemistry , cycloaddition , stereochemistry , mycobacterium tuberculosis , combinatorial chemistry , nuclear chemistry , organic chemistry , tuberculosis , catalysis , medicine , mathematical analysis , mathematics , pathology
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 0.50 μ g/mL.