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Bioorg Med Chem Lett. 2016 Jun 15;26(12):2907-2911. doi: 10.1016/j.bmcl.2016.04.045. Epub 2016 Apr 19.

In vitro evaluation of imidazo[4,5-c]quinolin-2-ones as gametocytocidal antimalarial agents.

Author information

1
National Center for Advancing Translational Sciences, National Institutes of Health, Bethesda, MD 20892, United States.
2
Department of Biology, Loyola University Chicago, Chicago, IL 60660, United States.
3
National Center for Advancing Translational Sciences, National Institutes of Health, Bethesda, MD 20892, United States. Electronic address: huangwe@mail.nih.gov.

Abstract

Novel imidazo[4,5-c]quinolin-2-ones were synthesized and evaluated in asexual blood stage and late stage gametocyte assays of Plasmodium falciparum, a major causative agent of malaria. The design of these compounds is based on a recently identified lead compound from a high throughput screen. A concise synthesis was developed that allowed for generation of analogues with substitution around both the quinoline and imidazolidinone rings. Through structure-activity relationship studies, a number of potent compounds were identified that possessed excellent antimalarial activity against both the asexual and sexual stages with minimal cytotoxicity in mammalian cells. This is the first Letter describing SAR and gametocytocidal activity of imidazo[4,5-c]quinolin-2-ones, a new lead series for malaria treatment and prevention.

KEYWORDS:

Antimalarial; Gametocytes; Gametocytocidal; Imidazo[4,5-c]quinolin-2-one; Plasmodium falciparum

PMID:
27156776
PMCID:
PMC4887403
DOI:
10.1016/j.bmcl.2016.04.045
[Indexed for MEDLINE]
Free PMC Article

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