title: Heterocyclic isosters of antimycobacterial salicylanilides.
abstract: 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.
authors.affiliation: Department of Inorganic and Organic Chemistry, Faculty of Pharmacy, Heyrovského 1203, CZ 500 05 Hradec Králové, Czech Republic.
authors.forename: Josef
authors.initials: J
authors.lastname: Matyk
authors.forename: Karel
authors.initials: K
authors.lastname: Waisser
authors.forename: Katerina
authors.initials: K
authors.lastname: Drazková
authors.forename: Jirí
authors.initials: J
authors.lastname: Kunes
authors.forename: Vera
authors.initials: V
authors.lastname: Klimesová
authors.forename: Karel
authors.initials: K
authors.lastname: Palát
authors.forename: Jarmila
authors.initials: J
authors.lastname: Kaustová
mesh_terms: 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
chemical_list: D000900:Anti-Bacterial Agents; D006571:Heterocyclic Compounds; D012457:Salicylamides