The oriented development of antituberculotics: salicylanilides.
On the basis of our previous results 22 salicylanilides were synthesized. The compounds were tested for in vitro antimycobacterial activity against Mycobacterium tuberculosis, Mycobacterium kansasii, and Mycobacterium avium. The Free-Wilson method was used to evaluate structure-antimycobacterial activity relationships. 4-Chloro-N-(4-propylphenyl)salicylamide and 5-chloro-N-(4-propylphenyl)salicylamide were selected for preclinical studies.
Waisser
Karel
K
Department of Inorganic and Organic Chemistry, Charles University in Prague, Faculty of Pharmacy, Hradec Králové, Czech Republic. waisser@faf.cuni.cz
Matyk
Josef
J
Divisová
Hana
H
Husáková
Petra
P
Kunes
Jirí
J
Klimesová
Vera
V
Kaustová
Jarmila
J
Möllmann
Ute
U
Dahse
Hans-Martin
HM
Miko
Milan
M
D000995:Antitubercular Agents / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology; D008826:Microbial Sensitivity Tests; D009162:Mycobacterium avium / Q000187:drug effects; D019909:Mycobacterium kansasii / Q000187:drug effects; D009169:Mycobacterium tuberculosis / Q000187:drug effects; D012458:Salicylanilides / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology; D013329:Structure-Activity Relationship
D000995:Antitubercular Agents; D012458:Salicylanilides