SYNTHESIS AND SOME PHYSICOCHEMICAL PROPERTIES OF Y-N-(3,4-DIMETHYL-5-ISOXAZOLYL)-1,4-NAPHTHOQUINONE 4-IMINE DERIVATIVES

Some derivatives of y-N-(3,4-dimethyl-5-isoxazolyl)-1,4-naphthoquinone 4-imine (3), a poorly soluble drug, were synthesized in an attempt to improve their physicochemical properties. The new compounds were char acterized by spectroscopic methods including an iterative NMR method ( the LAOCOON III program). The physicochemical properties such as solub ility, relative lipophilicity (R(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 ac tivity was also reported for some derivatives.