Search for new pharmacophores for antimalarial activity. Part II: Synthesis and antimalarial activity of new 6-ureido-4-anilinoquinazolines |
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Authors: | S. Madapa Z. Tusi A. Mishra K. Srivastava S.K. Pandey R. Tripathi S.K. Puri S. Batra |
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Affiliation: | 1. Medicinal and Process Chemistry Division, Central Drug Research Institute, PO Box 173, Lucknow 226001, India;2. Parasitology Division, Central Drug Research Institute, PO Box 173, Lucknow 226001, India |
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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. |
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