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

IR@CDRI: CSIR-Central Drug Research Institute, Lucknow

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Field Value
 
Creator Madapa, Sudharshan
Tusi, Zehra
Mishra, A
Srivastava, K
Pandey, S K
Tripathi, R
Puri, S K
Batra, Sanjay
 
Date 2010-03-02T06:08:42Z
2010-03-02T06:08:42Z
2009
 
Identifier Bioorganic & Medicinal Chemistry 17 (2009) 222–234
http://hdl.handle.net/123456789/519
 
Description 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
 
Format 240861 bytes
application/pdf
 
Language en
 
Relation CDRI Communication Number 7626
 
Title Search for new pharmacophores for antimalarial activity (Part II): Synthesis and antimalarial activity of new 6-ureido-4-anilinoquinazolines
 
Type Article