| Literature DB >> 23205265 |
Bryan T Mott1, Ken Chih-Chien Cheng, Rajarshi Guha, Valerie P Kommer, David L Williams, Jon J Vermeire, Michael Cappello, David J Maloney, Ganesha Rai, Ajit Jadhav, Anton Simeonov, James Inglese, Gary H Posner, Craig J Thomas.
Abstract
Parasitic diseases continue to have a devastating impact on human populations worldwide. Lack of effective treatments, the high cost of existing ones, and frequent emergence of resistance to these agents provide a strong argument for the development of novel therapies. Here we report the results of a hybrid approach designed to obtain a dual acting molecule that would demonstrate activity against a variety of parasitic targets. The antimalarial drug amodiaquine has been covalently joined with a nitric oxide-releasing furoxan to achieve multiple mechanisms of action. Using in vitro and ex vivo assays, the hybrid molecule shows activity against three parasites - Plasmodium falciparum, Schistosoma mansoni, and Ancylostoma ceylanicum.Entities:
Year: 2012 PMID: 23205265 PMCID: PMC3509744 DOI: 10.1039/C2MD20238G
Source DB: PubMed Journal: Medchemcomm ISSN: 2040-2503 Impact factor: 3.597