Čes. slov. farm. 2009, 58(5):203-207

Antimycobacterial activity of novel derivatives of arylcarbonyloxyaminopropanols

S. Kečkéšová^1,*, E. Sedlárová¹, J. Čižmárik¹, V. Garaj¹, J. Csöllei², P. Mokrý², F. Andriamainty¹, I. Malík¹, J. Kaustová³

¹ Comenius University, Faculty of Pharmacy, Department of Pharmaceutical Chemistry, Bratislava

² University of Veterinary and Pharmaceutical Sciences, Faculty of Pharmacy, Institute of Chemical Drugs, Brno

³ Regional Institute of Public Health, Ostrava

The study examined the antimicrobial activity of 2-hydroxy-3-[4-(2-fluoro, 4-fluoro, and 2-metoxyphenyl)-piperazin-1-yl]-propyl-4-[(alkoxycarbonyl)amino] benzoates, their salts with hydrochloric acid, with one to four carbon atoms in the alkoxy group of the carbamoyl group studied and described. The series of these substances were evaluated in vitro against Mycobacterium tuberculosis, Mycobacterium avium, Mycobacterium kansasii and against clinically isolated strains of Mycobacterium kansasii 6 509/96. The correlation of this activity with lipophilicity (log k') was used to describe the structure-antimycobacterial activity relationships (QSARs). The tests have shown that practically all the substances under study possess antituberculotic activity. In vitro antimycobacterial activity increased with increasing lipophilicity. According to the obtained results, the substances can be considered as potential antituberculotics.

Keywords: antimycobacterial activity; antituberculotic activity; potential antituberculotics; arylcarbonyloxyaminopropanols; lipophilicity; phenylcarbamates

Grants and funding:

This study was supported by the VEGA grant No. 1/4291/07.

Received: October 5, 2009; Accepted: November 4, 2009; Published: May 1, 2009  Show citation