Collect. Czech. Chem. Commun. 1993, 58, 205-212

Antituberculotic 4'-Cyclohexylthiobenzanilides: Combination of Free-Wilson Method in QSAR with Topliss Approach

Karel Waissera, Lenka Kubicováa and Želmíra Odlerováb

a Department of Inorganic and Organic Chemistry, Faculty of Pharmacy, Charles University, 501 65 Hradec Králové, Czech Republic
b Institute of Preventive and Clinical Medicine, 833 01 Bratislava, Slovak Republic


On the basis of a preliminary study of antimycobacterial activity of thiobenzanilides against Mycobacterium kansasii, a group of 4'-cyclohexylthiobenzanilids have been prepared which exhibit a significant activity against the microorganism mentioned. The whole set of 35 thiobenzanilides was tested with Mycobacterium tuberculosis, and on the basis of QSAR analysis conclusions have been made with regard to prognostics of structures suitable for further studies. The problem was solved by the method by Free and Wilson combined with the Topliss approach and by a Hansch type analysis.