Preparation and Antimalarial Activity of Water Soluble Derivatives of 6-Bromo-Alpha-(di-n-heptylaminomethyl)-9-phenanthrenemethanol

摘要

In an effort to overcome the problem of water insolubility encountered with 6-bromo-alpha-(di-n-heptylaminomethyl)-9-phenanthrene-methanol, an effective antimalarial, several derivatives were prepared. These included dicarboxylic acid salts, half esters and esters. The distribution coefficients of the parent compound hydrochloride and these derivatives between n-octanol and water were determined using uv spectroscopy. These data indicated that none of the dicarboxylic acid salts, half esters or esters was more water soluble than the parent compound hydrochloride. However, antimalarial activity data against Plasmodium berghei indicated that some of these derivatives were slightly more active than the parent compound. Apparently, there was no correlation between the water solubility and antimalarial activity of these derivatives. (Author)