"Synthesis and some physicochemical properties of 2-hydroxy-N-(3,4-dimethyl-5-isoxazolyl)-1,4-naphthoquinone-4-imine derivatives

NR SPERANDEO

JOURNAL OF PHARMACEUTICAL SCIENCES

JOHN WILEY & SONS INC

Año: 1994 vol. 83 p. 332 - 332

0022-3549

ome derivatives of 2-hydroxy-N(3,4-dimethyl-5-isoxazolyl)-1,4-naphthoquinone 4-imine (3), a poorly soluble drug, weresynthesized in an attempt to improve their physicochemical properties.The new compounds were characterized by spectroscopic methodsincluding an iterative NMR method (the LAOCOON 111 program). Thephysicochemical properties such as solubility, relative lipophilicity (RM),and partition coefficients (Leo-Hansch fragmental system) weredetermined. Some derivatives were more iipophilic than 3 and onewas water soluble. In vitro antibacterial activity was also reportedfor some derivatives.