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| Title: | Search for new pharmacophores for antimalarial activity (Part II): Synthesis and antimalarial activity of new 6-ureido-4-anilinoquinazolines |
| Authors: | Madapa, Sudharshan
Tusi, Zehra
Mishra, A
Srivastava, K
Pandey, S K
Tripathi, R
Puri, S K
Batra, Sanjay |
| Issue Date: | 2009 |
| Citation: | Bioorganic & Medicinal Chemistry 17 (2009) 222–234 |
| Series/Report no.: | CDRI Communication Number 7626 |
| 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 g/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 discovey of one analog (30g) displaying 40% curative activity (28 days) against mdr P. yoeilli nigeriensis at an oral dose of 100mg/kg x 4days |
| URI: | http://hdl.handle.net/123456789/519 |
| Appears in Collections: | Medicinal and Process Chemistry
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| sbatra-7626-bmc-2009-224.pdf | | 235Kb | Adobe PDF | View/Open |
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