A furoxan-amodiaquine hybrid as a potential therapeutic for three parasitic diseases

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^*

来源：Medchemcomm, 2012, 3(12): 1505-1511.

DOI：10.1039/c2md20238g

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.

• 出版日期2012-12