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2H-l,3-Benzoxazine-2,4(3H)-diones Substituted in Position 6 as Antimycobacterial Agents

K. Waisser, J. Hladůvková, P. Holý, M. Macháček, P. Karajannis, L. Kubicová, V. Klimešová, J. Kuneš, and J. Kaustová

Department of Inorganic and Organic Chemistry, Charles University in Prague, Faculty of Pharmacy in Hradec Králové, CZ-500 05 Hradec Králové

 

Abstract: Cyclization of salicylanilides substituted in position 5 gave the corresponding 3-(R-phenyl)-2H-1,3-benzoxazine-2,4(3H)-diones substituted in position fi. Their minimum inhibition concentrations against Mycobacterium tuberculosis, M. kansasii, and M. avium are reported. Most of the studied compounds possess activity against M. kansasii and M. avium greater than Isoniazid. The antimycobacterial profile of the compounds was evaluated according to the criteria based on vector algebra, such as cosine coefficient. Quantitative structure-activity relationships were analyzed by the Free-Wilson and Hansch method. The antimycobacterial activity increases with increasing electron-accepting ability and lipophilicity of the substituents on the phenyl ring, whereas the effect of substituents in the 6 position seems to be more complex.

Full paper in Portable Document Format: 555a323.pdf

 

Chemical Papers 55 (5) 323–334 (2001)

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