Back
Full-text
Journal article

Identification and optimization of an aminoalcohol-carbazole series with antimalarial properties.

  • Molette J Merck Serono, 9 chemin des mines, 1202 Geneva, Switzerland.
  • Routier J Merck Serono, 9 chemin des mines, 1202 Geneva, Switzerland.
  • Abla N Merck Serono, 9 chemin des mines, 1202 Geneva, Switzerland.
  • Besson D Special Program for Research & Training in Tropical Diseases (TDR), World Health Organization , Avenue Appia 20, 1211 Geneva 27, Switzerland.
  • Bombrun A Merck Serono, 9 chemin des mines, 1202 Geneva, Switzerland.
  • Brun R Swiss Tropical and Public Health Institute, Socinstrasse. 57, 4051 Basel, Switzerland , and University of Basel, Petersplatz 1, 4003 Basel, Switzerland.
  • Burt H Merck Serono, 9 chemin des mines, 1202 Geneva, Switzerland.
  • Georgi K Merck Serono, 9 chemin des mines, 1202 Geneva, Switzerland.
  • Kaiser M Swiss Tropical and Public Health Institute, Socinstrasse. 57, 4051 Basel, Switzerland , and University of Basel, Petersplatz 1, 4003 Basel, Switzerland.
  • Nwaka S Special Program for Research & Training in Tropical Diseases (TDR), World Health Organization , Avenue Appia 20, 1211 Geneva 27, Switzerland.
  • Muzerelle M Merck Serono, 9 chemin des mines, 1202 Geneva, Switzerland.
  • Scheer A Merck Serono, 9 chemin des mines, 1202 Geneva, Switzerland.
Show more…
  • 2014-06-06
Published in:
  • ACS medicinal chemistry letters. - 2013
IC50
Malaria
Plasmodium berghei
Plasmodium falciparum
SAR
WHO
carbazole
hERG
English Recent observations on the emergence of artemisinin resistant parasites have highlighted the need for new antimalarial treatments. An HTS campaign led to the identification of the 1-(1-aminopropan-2-ol)carbazole analogues as potent hits against Plasmodium falciparum K1 strain. The SAR study and optimization of early ADME and physicochemical properties direct us to the selection of a late lead compound that shows good efficacy when orally administrated in the in vivo P. berghei mouse model.
Language
  • English
Open access status
green
Identifiers
Persistent URL
https://sonar.rero.ch/global/documents/114417
Statistics
Document views: 68 File downloads:
  • Full-text: 0