Sulfonyl-phenyl-ureido benzamidines; a novel structural class of potent antimalarial agents

Bioorg Med Chem Lett. 2004 Apr 19;14(8):1979-82. doi: 10.1016/j.bmcl.2004.01.083.

Abstract

The high throughput in silico screening of a virtual library into the structure of the P. falciparum lactate dehydrogenase (LDH) with the 4SCan technology yielded a series of biphenyl urea compounds. These were chemically optimized to a new structural class of potent antimalarial agents. The compounds did not inhibit plasmodium LDH enough to fully explain their potency. Therefore we conclude that an unknown mode of action may be the cause of the antimalarial activity.

MeSH terms

  • Animals
  • Antimalarials / chemical synthesis
  • Antimalarials / chemistry*
  • Antimalarials / pharmacology*
  • Benzamidines / chemical synthesis
  • Benzamidines / chemistry*
  • Benzamidines / pharmacology*
  • Drug Evaluation, Preclinical
  • L-Lactate Dehydrogenase / antagonists & inhibitors*
  • Plasmodium falciparum / drug effects
  • Plasmodium falciparum / enzymology
  • Protozoan Proteins / antagonists & inhibitors
  • Structure-Activity Relationship

Substances

  • Antimalarials
  • Benzamidines
  • Protozoan Proteins
  • L-Lactate Dehydrogenase