1376766-59-4Relevant articles and documents
Primaquine-pyrimidine hybrids: Synthesis and dual-stage antiplasmodial activity
Kaur, Hardeep,Machado, Marta,De Kock, Carmen,Smith, Peter,Chibale, Kelly,Prudêncio, Miguel,Singh, Kamaljit
, p. 266 - 273 (2015/07/08)
Abstract A series of novel pyrimidine-primaquine hybrids were synthesized and their effectiveness against the blood and liver stages of malaria parasites was evaluated. The hybrids displayed enhanced liver stage in vitro activity against P. berghei liver
2-Aminopyrimidine based 4-aminoquinoline anti-plasmodial agents. Synthesis, biological activity, structure-activity relationship and mode of action studies
Singh, Kamaljit,Kaur, Hardeep,Chibale, Kelly,Balzarini, Jan,Little, Susan,Bharatam, Prasad V.
, p. 82 - 97 (2012/08/08)
2-Aminopyrimidine based 4-aminoquinolines were synthesized using an efficacious protocol. Some of the compounds showed in vitro anti-plasmodial activity against drug-sensitive CQS (3D7) and drug-resistant CQ R (K1) strains of Plasmodium falciparum in the nM range. In particular, 5-isopropyloxycarbonyl-6-methyl-4-(2-nitrophenyl)-2-[(7- chloroquinolin-4-ylamino)butylamino] pyrimidine depicted the lowest IC 50 (3.6 nM) value (56-fold less than CQ) against CQR strain. Structure-activity profile and binding with heme, μ-oxo-heme have been studied. Binding assays with DNA revealed better binding with target parasite type AT rich pUC18 DNA. Most compounds were somewhat cytotoxic, but especially cytostatic. Molecular docking analysis with Pf DHFR allowed identification of stabilizing interactions.