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.
A furoxan-amodiaquine hybrid as a potential therapeutic for three parasitic diseases().
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作者:Mott Bryan T, Cheng Ken Chih-Chien, Guha Rajarshi, Kommer Valerie P, Williams David L, Vermeire Jon J, Cappello Michael, Maloney David J, Rai Ganesha, Jadhav Ajit, Simeonov Anton, Inglese James, Posner Gary H, Thomas Craig J
| 期刊: | Medchemcomm | 影响因子: | 0.000 |
| 时间: | 2012 | 起止号: | 2012 Dec;3(12):1505-1511 |
| doi: | 10.1039/C2MD20238G | ||
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