Local parameters in the studies of structure--antimycobacterial activity of potential antituberculotics

Karel Waisser (waisser@faf.cuni.cz), Milan Peřina

Department of Inorganic and Organic Chemistry, Charles University in Prague, Faculty of Pharmacy in Hradec Králové, Czech Republic

Summary

The examples presented in this paper aim to demonstrate that values of physico-chemical (local) parameters of molecular fragments could correlate with the final biological activity. This approach can provide equations, which in their formal aspect resemble of the Hansch but operate with local parameters. The examples presented in the study concern antimycobacterial activity (3-phenyl-2H-1,3-benzoxazine-2,4(3H)-diones, 7-benzo[c]fluorenones, hydrindacenes, thioanilides, salicylanilides) that was the principal aim of our research. We are using the locale parameters for the study of another group of compounds now (N-benzylsalicylamides and esters of alkoxysubstituted phenylcarbamoic acid).