QSAR Analysis of Antimycobacterial N-pyridinylsalicylamides

Karel Waisser (waisser@faf.cuni.cz), Kateřina Dražková, Josef Matyk, Karel Palát

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

Summary

The Free-Wilson approach was used for QSAR study. The molecules were separated on the heterocyclic and salicyl moieties of the molecules. The 2-pyridyl moiety increases the antimycobacterial activity more then the 3- or 4- pyridyl moiety. Substitution of the salicyl moiety by chlorine in position 4 or 5, and 2-pyridyl moiety by nitro group or by bromine in position 5 had the strongest influence on the increasis of antimycobacterial activity. N-Pyridinylsalicylamides constitute a new group of potential antituberculotics. The compounds under study are more active than INH against potentially pathogenic strains.