title: Antibacterial action of amphipathic derivatives of isoniazid against the Mycobacterium avium complex.
abstract: The antibacterial action of amphipathic derivatives of isoniazid (INH) as compared to the parent hydrophilic molecule was determined against the bacteria of the Mycobacterium avium complex (MAC) using a 7H11 agar-dilution method. The results obtained showed a higher activity of 1-isonicotinyl-2-palmitoyl hydrazine and 1-isonicotinyl-2-(12 hydroxy dodecanoyl) hydrazine as compared to INH. However, when one mannose residue was terminally attached to the fatty acid chain of the latter, it lost its anti-MAC activity. 1-isonicotinyl-2-D-galacturonic acid hydrazone (but not hydrazine) also showed increased activity against MAC. Although pristinamycin was shown to bind to M. avium surface lipids, the INH-pristinamycin derivative was not more active than INH alone. These findings are discussed in respect to a proposed mechanism of diffusion across a lipid barrier.
authors.affiliation: Unité de la Tuberculose et des Mycobactéries, Institut Pasteur, Paris, France.
authors.forename: N
authors.initials: N
authors.lastname: Rastogi
authors.forename: B
authors.initials: B
authors.lastname: Moreau
authors.forename: M L
authors.initials: ML
authors.lastname: Capmau
authors.forename: K S
authors.initials: KS
authors.lastname: Goh
authors.forename: H L
authors.initials: HL
authors.lastname: David
mesh_terms: D000900:Anti-Bacterial Agents; D007202:Indicators and Reagents; D007538:Isoniazid / Q000031:analogs & derivatives* / Q000138:chemical synthesis / Q000494:pharmacology*; D008826:Microbial Sensitivity Tests; D009162:Mycobacterium avium / Q000187:drug effects* / Q000254:growth & development; D013329:Structure-Activity Relationship
chemical_list: D000900:Anti-Bacterial Agents; D007202:Indicators and Reagents; D007538:Isoniazid