Search for new pharmacophores for antimalarial activity. Part II: Synthesis and antimalarial activity of new 6-ureido-4-anilinoquinazolines

S. Madapa, Z. Tusi, A. Mishra, K. Srivastava, S. K. Pandey, R. Tripathi, S. K. Puri, S. Batra

Research output: Contribution to journalArticlepeer-review

102 Scopus citations

Abstract

Synthesis of new 6-ureido-4-anilinoquinazolines have been accomplished and their in vitro antimalarial activity against chloroquine-sensitive P. falciparum have been examined. Out of 64 compounds evaluated, the IC50 of 16 compounds which have displayed MIC of 0.25 μg/mL were also recorded. One of the compounds (24g) had IC50 value of 2.27 ng/mL which was equipotent to the standard drug chloroquine used in the bioassay. The in vivo evaluation of a few compounds among the series led to discovery of one analog (30g) displaying 40% curative activity (28 days) against mdr P. yoeilli nigeriensis at an oral dose of 100 mg/kg × 4days.

Original languageEnglish
Pages (from-to)222-234
Number of pages13
JournalBioorganic and Medicinal Chemistry
Volume17
Issue number1
DOIs
StatePublished - 1 Jan 2009
Externally publishedYes

Keywords

  • Antimalarial
  • In vitro
  • In vivo
  • P. falciparum
  • Quinazoline
  • Urea

ASJC Scopus subject areas

  • Biochemistry
  • Molecular Medicine
  • Molecular Biology
  • Pharmaceutical Science
  • Drug Discovery
  • Clinical Biochemistry
  • Organic Chemistry

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