Search for new pharmacophores for antimalarial activity. Part III: synthesis and bioevaluation of new 6-thioureido-4-anilinoquinazolines.
Syntheses and in vitro antimalarial evaluation of 42 new thioureidoquinazolines have been carried out. Several analogs showed promising antimalarial effect in the in vitro investigation against chloroquine-sensitive 3D7 strain of Plasmodium falciparum whereas one of the compounds shows 50% curative effect in the mouse model at an oral dose of 100mg/kg x 4 days against multidrug resistant Plasmodium yoelii nigeriensis.
Mishra
A
A
Medicinal and Process Chemistry Division, Central Drug Research Institute, Lucknow 226001, India.
Srivastava
K
K
Tripathi
R
R
Puri
S K
SK
Batra
S
S
D000818:Animals; D000962:Antimalarials / Q000138:chemical synthesis* / Q000494:pharmacology / Q000627:therapeutic use*; D002470:Cell Survival / Q000187:drug effects; D002522:Chlorocebus aethiops; D005260:Female; D008288:Malaria / Q000188:drug therapy*; D008297:Male; D051379:Mice; D015394:Molecular Structure; D021261:Parasitic Sensitivity Tests; D010963:Plasmodium falciparum / Q000187:drug effects; D010967:Plasmodium yoelii / Q000187:drug effects; D011799:Quinazolines / Q000138:chemical synthesis* / Q000494:pharmacology / Q000627:therapeutic use*; D013329:Structure-Activity Relationship; D013890:Thiourea / Q000138:chemical synthesis* / Q000494:pharmacology / Q000627:therapeutic use*; D014709:Vero Cells
D000962:Antimalarials; D011799:Quinazolines; D013890:Thiourea