id	author	title	date	pages	extension	mime	words	sentences	flesch	summary	cache	txt
cord-304375-l5gvpat3	Singh, Kamaljit	2-Aminopyrimidine based 4-aminoquinoline anti-plasmodial agents. Synthesis, biological activity, structure–activity relationship and mode of action studies	2012-03-13		.txt	text/plain	6588	381	55	Some of the compounds showed in vitro anti-plasmodial activity against drug-sensitive CQ(S) (3D7) and drug-resistant CQ(R) (K1) strains of Plasmodium falciparum in the nM range. In this communication, we report synthesis of a set of compounds that possess basic, hydrophobic as well as hydrogen bonding substituents, required for targeting either or both heme as well as DNA, thus providing new antimalarial agents active against chloroquine resistant strains of P. We have evaluated their anti-plasmodial activity, cytotoxicity and cytostatic activity, binding studies with DNA and heme (monomeric as well as m-oxo dimeric) using UVevisible, fluorescence spectrophotometry as well as NMR analysis. The comparison of association constants of 10r and 10c for monomeric and m-oxo heme reveals that both compounds bind strongly with m-oxo heme than monomeric heme and inhibit hemozoin formation by blocking the growing face of heme resulting in the observed anti-plasmodial activity.	./cache/cord-304375-l5gvpat3.txt	./txt/cord-304375-l5gvpat3.txt