Correlation of fungostatic activity with log P and sigma parameters in the group of thiobenzanilides.
2,4-Dihydroxythiobenzanilide and its analogues were recently found to show strong biological activity. Earlier works exhibited that their biological activity depends strongly on their lipophilicity determined by means of RP-HPLC. Among others, fungostatic activity against tested yeast and mould strains appeared to be comparatively poorer modelled by chromatographic lipophilicity parameters. Very high correlation (r approximately 0.85-0.9) with these activities was obtained by means of multiparameter regression analysis where calculated log P and Hammet sigma values were involved as the independent variables. Analysed data show that activity against yeast and mould fungi is a superposition of two basic properties of thiobenzanilides: their lipophilicity and electronic properties.
Jóźwiak
K
K
Department of Inorganic and Analytical Chemistry, Medical University, 6 Staszica Str., 20-081 Lublin, Poland.
Szumiło
H
H
D000813:Anilides / Q000494:pharmacology; D000935:Antifungal Agents / Q000737:chemistry / Q000494:pharmacology*; D002851:Chromatography, High Pressure Liquid; D021281:Quantitative Structure-Activity Relationship; D012044:Regression Analysis; D012995:Solubility
D000813:Anilides; D000935:Antifungal Agents; C034595:benzanilide