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ID: ALA2010777

Journal: Bioorg Med Chem Lett

Title: Synthesis and evaluation of human phosphodiesterases (PDE) 5 inhibitor analogs as trypanosomal PDE inhibitors. Part 2. Tadalafil analogs.

Authors: Ochiana SO, Gustafson A, Bland ND, Wang C, Russo MJ, Campbell RK, Pollastri MP.

Abstract: In this Letter we describe our ongoing target repurposing efforts focused on discovery of inhibitors of the essential trypanosomal phosphodiesterase TbrPDEB1. This enzyme has been implicated in virulence of Trypanosoma brucei, the causative agent of human African trypanosomiasis (HAT). We outline the synthesis and biological evaluation of analogs of tadalafil, a human PDE5 inhibitor currently utilized for treatment of erectile dysfunction, and report that these analogs are weak inhibitors of TbrPDEB1.

CiteXplore: 22377518

DOI: 10.1016/j.bmcl.2012.01.118