Accession Number : AD0734362
Title : Synthesis of Organic Compounds for Malaria Chemotherapeutic Studies.
Descriptive Note : Annual progress rept. no. 6, 1 Jun 70-31 Jul 71,
Corporate Author : MIDWEST RESEARCH INST KANSAS CITY MO
Personal Author(s) : Cheng,C. C. ; Chien,Ping-Lu ; McCaustland,D. J. ; Burton,William H.
Report Date : SEP 1971
Pagination or Media Count : 53
Abstract : The work reported herein consists of an investigation of a structure-activity relationship study on side chain modification of substituted phenanthrene aminoalcohols. During the present report period, a total of 29 compounds have been synthesized, characterized, and submitted for antimalarial evaluation. A number of these have shown curative activity against Plasmodium berghei and P. gallinaceum. Among these compounds, 3,6-bis(trifluoromethyl)-alpha (1-propylbutylaminomethyl)-9-phenanthrenemethanol hydrochloride (WR-167619; AX-29812) was found to possess a 17.7 day activity at 10 mg/kg and is curative at 20 mg/kg against P. berghei. Activity of 3,6-bis(trifluoromethyl)-alpha-(butylaminomethyl)-9-phenanthrenemethanol hydrochloride (WR-165543; AX-27845) is comparable. (Author)
Descriptors : (*ANTIMALARIALS, SYNTHESIS(CHEMISTRY)), MOLECULAR STRUCTURE, HALOGENATED HYDROCARBONS, PHENANTHRENES, METHANOLS, AMINES, PYRIDINES, FLUORINE COMPOUNDS, BROMINE COMPOUNDS, CHLORINE COMPOUNDS, PIPERIDINES
Subject Categories : Pharmacology
Distribution Statement : APPROVED FOR PUBLIC RELEASE