Design, synthesis and evaluation of 5-substituted ...[Bioorg Med Chem Lett. 2005]

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1: Bioorg Med Chem Lett. 2005 Jan 3;15(1):73-6. Links

Design, synthesis and evaluation of 5-substituted amino-2,4-diamino-8-chloropyrimido-[4,5-b]quinolines as novel antimalarials.

Joshi AA, Narkhede SS, Viswanathan CL.

Department of Pharmaceutical Chemistry, Bombay College of Pharmacy, Kalina, Santacruz (E), Mumbai 400 098, India. joshiadvait78@yahoo.com

Novel 5-substituted amino-2,4-diamino-8-chloropyrimido-[4,5-b]quinolines were designed based on a pharmacophore developed for potent antimalarial activity using Chem-X and MOE softwares. The designed molecules were synthesized by following a novel route and were evaluated by Rane's test for blood schizonticidal activity in mice infected by Plasmodium berghei. Based on the Mean Survival Time (MST) data, of the nine compounds evaluated, three had curative potential when compared with chloroquine.

PMID: 15582413 [PubMed - indexed for MEDLINE]

Docking studies and development of novel 5-heteroarylamino-2,4-diamino-8-chloropyrimido-[4,5-b]quinolines as potential antimalarials. [Bioorg Med Chem Lett. 2006]
Synthesis of quinolinyl chalcones and evaluation of their antimalarial activity. [Eur J Med Chem. 2001]
Novel aryl-bis-quinolines with antimalarial activity in-vivo. [J Pharm Pharmacol. 1998]
Review[Recent advances in the study of artemisinin-related 1,2,4-trioxanes and ozonides (1,2,4-trioxolanes) as antimalarials] [Yao Xue Xue Bao. 2005]
ReviewRecent developments in naturally derived antimalarials: cryptolepine analogues. [J Pharm Pharmacol. 2007]

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Design, synthesis and evaluation of 5-substituted amino-2,4-diamino-8-chloropyrimido-[4,5-b]quinolines as novel antimalarials.

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