Search for new pharmacophores for antimalrial activity (Part I): Synthesis and antimalarial activity of new 2-methyl-6-ureido-4-quinolinamides

Abstract

A total of 80 new 2-methyl-6-ureido-4-quinolinamides were synthesized and evaluated for their anitmalarial activity. Several analogs elicited the antimalarial effect at MIC of 0.25 mg/mL against the chlooquine-sensitive P. falciparum strain. The IC50 values of the active compounds were observed to be in ng/mL range and two of the analogs have better IC50 value than the standard chloroquine. In the in vivo assay against mdr CQ resistant P.yoelii N67/ P. yoeilli nigeriensis, however, none of the compound showed complete suppression of parasitaemia on day 7. One of the compounds displayed significant antibacterial effect against several strains of bacteria and was many-fold better than the standard drug gentamicin.