Heterocyclic isosters of antimycobacterial salicylanilides.
A series of 64 derivatives of substituted heterocyclic analogues of salicylanilides was synthesized. The compounds were evaluated for in vitro antimycobacterial activity against Mycobacterium tuberculosis, Mycobacterium avium and two strains of Mycobacterium kansasii. For the QSAR study, the combination of Free-Wilson approach with Hansch approach was used. The molecules were separated on the heterocyclic and salicyl moieties and the study of influences of electronic and hydrophobic properties was used as well. The compounds are a new group of potential anti-tuberculotics.
Matyk
Josef
J
Department of Inorganic and Organic Chemistry, Faculty of Pharmacy, Heyrovského 1203, CZ 500 05 Hradec Králové, Czech Republic.
Waisser
Karel
K
Drazková
Katerina
K
Kunes
Jirí
J
Klimesová
Vera
V
Palát
Karel
K
Kaustová
Jarmila
J
D000900:Anti-Bacterial Agents / Q000138:chemical synthesis* / Q000494:pharmacology; D002626:Chemistry, Pharmaceutical / Q000379:methods; D006571:Heterocyclic Compounds / Q000138:chemical synthesis* / Q000494:pharmacology; D008826:Microbial Sensitivity Tests / Q000379:methods; D012457:Salicylamides / Q000138:chemical synthesis* / Q000494:pharmacology
D000900:Anti-Bacterial Agents; D006571:Heterocyclic Compounds; D012457:Salicylamides