Accession Number : AD0758928

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

Descriptive Note : Rept. no. 2 (Final),

Corporate Author : WESTERN MICHIGAN UNIV KALAMAZOO

Personal Author(s) : Harmon,Robert E.

Report Date : 20 FEB 1973

Pagination or Media Count : 18

Abstract : 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)

Descriptors :   (*PHENANTHRENES, SYNTHESIS(CHEMISTRY)), (*ANTIMALARIALS, PHENANTHRENES), SOLUBILITY, BROMINE COMPOUNDS, CARBINOLS, HALOGENATED HYDROCARBONS, HYDROLYSIS, PHOSPHATES, PHOSPHORUS COMPOUNDS, PLASMODIUM

Subject Categories : Pharmacology
      Organic Chemistry

Distribution Statement : APPROVED FOR PUBLIC RELEASE