Antimycobacterial salicylanilides and 3-phenyl-2H-1,3-benzoxazine-2,4(3H)-diones
Authors:
K. Waisser; J. Gregor; P. Holý; L. Kubicová; V. Klimešová; J. Kaustová 1
Authors‘ workplace:
Katedra anorganické a organické chemie Farmaceutické fakulty Univerzity Karlovy, Hradec Králové, Krajská hygienická stanice, Ostrava
Published in:
Čes. slov. Farm., 2001; , 148-152
Category:
Overview
Salicylanilides and 3-phenyl-2H-1,3-benzoxazine-2,4(3H)-diones are strong antimycobacterial substances which can be considered to be potential antituberculotics. In order to be able to verify theprognostics of the relationships between the structure and antimycobacterial activity, the series ofpreviously evaluated substances was extended to include 4´-ethoxycarbonylsalicylanilide, 4´-tri-fluoromethylsalicylanilide, 4´-cyanidosalicylanilide, 4´-thiocarbamoylsalicylanilide, 3-(4-ethoxycar-bonylphenyl)-2H-1,3-benzoxazine-2,4(3H)-dione, 3-(4-trifluoromethylphenyl)-2H-1,3-benzoxazine--2,4(3H)-dione, and 3-(4-cyanidophenyl)-2H-1,3-benzoxazine-2,4-(3H)-dione. The substances wereevaluated against Mycobacterium tuberculosis, M. kansasii, and M. avium. In harmony with theprevious study (see ref. 1), antimycobacterial activity increased with increasing lipophilicity andelectron-acceptor properties of substituents. As the values of regression coefficients were notsubstantially changed after the complementation of the group, the present authors consider theproblem under study to be solved.
Key words:
salicylanilides - benzoxazine -Œ mycobacterium - tuberculostatic - QSAR
Labels
Pharmacy Clinical pharmacologyArticle was published in
Czech and Slovak Pharmacy
2001 Issue 3
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