Synthesis and Some Physicochemical Properties of 2-Hydroxy-AK3,4-dimethyl-5-isoxazolyl)-1,4-naphthoquinone 4-1 mine Derivatives

Some derivatives of 2-hydroxy-AA(3,4-dimethyl-5-isoxazol- yl}-1,4-naphthoquinone 4-imine (3), a poorly soluble drug, were synthesized in an attempt to improve their physicochemical properties. The new compounds were characterized by spectroscopic methods including an iterativenmR method (the LAOCOON III program). The physicochemical properties such as solubility, relative lipophilicity (/?M)< and partition coefficients (Leo-Hansch fragmental system) were determined. Some derivatives were more lipophilic than 3 and one was water soluble. In vitro antibacterial activity was also reported for some derivatives.