Antileishmanial bis-arylimidamides: DB766 analogs modified in the linker region and bis-arylimidamide structure–activity relationships

…, AA Farahat, X Zhu, T Pandharkar, DW Boykin…

文献索引：Reid, Carolyn S.; Zhu, Xiaohua; Pandharkar, Trupti; Werbovetz, Karl A.; Farahat, Abdelbasset A.; Boykin, David W. Bioorganic and Medicinal Chemistry Letters, 2012 , vol. 22, # 22 p. 6806 - 6810,5

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被引用次数: 11

摘要

Analogs of the lead antileishmanial bis-arylimidamide DB766 were prepared that possess unsymmetrical substitutions on the diphenylfuran linker, and an additional compound was synthesized that contains isopropoxy groups meta to the central furan. These agents all displayed nanomolar in vitro potency against intracellular Leishmania with selectivity indexes> 100 compared to J774 macrophages. While the unsymmetrical analogs were ...