Synthesis of Organic Compounds for Malaria Chemotherapeutic Studies.

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)

Document Details

Document Type
Technical Report
Publication Date
Sep 01, 1971
Accession Number
AD0734362

Entities

People

  • C. C. Cheng
  • D. J. Mccaustland
  • Ping-lu Chien
  • William H. Burton

Organizations

  • MRIGlobal

Tags

DTIC Thesaurus Topics

  • Antimalarials
  • Aromatic Compounds
  • Aromatic Hydrocarbons
  • Arthropod Borne Diseases
  • Bacterial Infections And Mycoses
  • Chemical Compounds
  • Cyclic Compounds
  • Diseases And Disorders
  • Hydrocarbons
  • Infectious Diseases
  • Malaria
  • Mosquito Borne Diseases
  • Organic Compounds
  • Parasitic Diseases
  • Phenanthrenes
  • Polycyclic Compounds
  • Test And Evaluation

Fields of Study

  • Chemistry

Readers

  • Parasitology and Pharmacology of Malaria.