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Bioorg Med Chem Lett. 2012 Apr 1;22(7):2579-81. doi: 10.1016/j.bmcl.2012.01.119. Epub 2012 Feb 9.

Synthesis and evaluation of human phosphodiesterases (PDE) 5 inhibitor analogs as trypanosomal PDE inhibitors. Part 1. Sildenafil analogs.

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1
Northeastern University Department of Chemistry & Chemical Biology, 417 Egan Research Center, 360 Huntington Avenue, Boston, MA 02115, USA.

Abstract

Parasitic diseases, such as African sleeping sickness, have a significant impact on the health and well-being in the poorest regions of the world. Pragmatic drug discovery efforts are needed to find new therapeutic agents. In this Letter we describe target repurposing efforts focused on trypanosomal phosphodiesterases. We outline the synthesis and biological evaluation of analogs of sildenafil (1), a human PDE5 inhibitor, for activities against trypanosomal PDEB1 (TbrPDEB1). We find that, while low potency analogs can be prepared, this chemical class is a sub-optimal starting point for further development of TbrPDE inhibitors.

PMID:
22370268
PMCID:
PMC3307826
DOI:
10.1016/j.bmcl.2012.01.119
[Indexed for MEDLINE]
Free PMC Article
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