title: Relationship between the structure and antimycobacterial activity of substituted salicylanilides.
abstract: A series of 143 salicylanilides substituted in positions 4 and 5 and in positions 3' and 4' was synthesized. The compounds were evaluated for in vitro antimycobacterial activity against Mycobacterium tuberculosis, Mycobacterium kansasii, and Mycobacterium avium. To describe the structure-antimycobacterial activity relationships (QSARs), an approach based on the combination of the Free-Wilson and Hansch methods was employed (the substituent constants were used in the case of the substituents on the phenyl ring; indicator parameters were used for the substituents on the acyl moiety). The relationships between the antimycobacterial activity and physico-chemical parameters of all substituents were also explored. The quadratic representation of lipophilicity parameters did not lead to significant correlations.
authors.affiliation: Department of Inorganic and Organic Chemistry, Faculty of Pharmacy, Heyrovského 1203, CZ 500 05 Hradec Králové, Czech Republic. waisser@faf.cuni.cz
authors.forename: Karel
authors.initials: K
authors.lastname: Waisser
authors.forename: Otakar
authors.initials: O
authors.lastname: Bures
authors.forename: Pavel
authors.initials: P
authors.lastname: Holý
authors.forename: Jirí
authors.initials: J
authors.lastname: Kunes
authors.forename: Radek
authors.initials: R
authors.lastname: Oswald
authors.forename: Lucie
authors.initials: L
authors.lastname: Jirásková
authors.forename: Milan
authors.initials: M
authors.lastname: Pour
authors.forename: Vera
authors.initials: V
authors.lastname: Klimesová
authors.forename: Lenka
authors.initials: L
authors.lastname: Kubicová
authors.forename: Jarmila
authors.initials: J
authors.lastname: Kaustová
mesh_terms: D000900:Anti-Bacterial Agents / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology; D008826:Microbial Sensitivity Tests; D009161:Mycobacterium / Q000187:drug effects*; D012458:Salicylanilides / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology*; D013329:Structure-Activity Relationship
chemical_list: D000900:Anti-Bacterial Agents; D012458:Salicylanilides