141333-36-0Relevant articles and documents
Repurposing human PDE4 inhibitors for neglected tropical diseases: Design, synthesis and evaluation of cilomilast analogues as Trypanosoma brucei PDEB1 inhibitors
Amata, Emanuele,Bland, Nicholas D.,Hoyt, Charles T.,Settimo, Luca,Campbell, Robert K.,Pollastri, Michael P.
supporting information, p. 4084 - 4089 (2014/09/29)
A medicinal chemistry exploration of the human phosphodiesterase 4 (hPDE4) inhibitor cilomilast (1) was undertaken in order to identify inhibitors of phosphodiesterase B1 of Trypanosoma brucei (TbrPDEB1). T. brucei is the parasite which causes African sleeping sickness, a neglected tropical disease that affects thousands each year, and TbrPDEB1 has been shown to be an essential target of therapeutic relevance. Noting that 1 is a weak inhibitor of TbrPDEB1, we report the design and synthesis of analogs of this compound, culminating in 12b, a sub-micromolar inhibitor of TbrPDEB1 that shows modest inhibition of T. brucei proliferation.
METHOD FOR PREPARING SUBSTITUTED 4-PHENYL-4-CYANOCYCLOHEXANOIC ACIDS
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, (2008/06/13)
This invention relates to a method of preparing a compound type where at least one of R′ or R″ is a carboxyl group (I) by treating a compound of formula (II) with a Group I(a) or Group II(a) metal halide, with an aprotic dipolar amide-based solvent and wa
Synthesis and biological evaluation of imidazol-2-one and 2-cyanoiminoimidazole derivatives: novel series of PDE4 inhibitors.
Andres, J Ignacio,Alonso, Jose M,Diaz, Adolfo,Fernandez, Javier,Iturrino, Laura,Martinez, Pedro,Matesanz, Encarna,Freyne, Eddy J,Deroose, Frederik,Boeckx, Gustaaf,Petit, Davy,Diels, Gaston,Megens, Anton,Somers, Marijke,Van Wauwe, Jean,Stoppie, Paul,Cools, Marina,De Clerck, Fred,Peeters, Danielle,de Chaffoy, Didier
, p. 653 - 658 (2007/10/03)
This communication describes the synthesis and in vitro PDE4 inhibitory activity of a novel series of imidazol-2-one and 2-cyanoiminoimidazole derivatives. The compounds described were also tested in in vivo models to evaluate their anti-inflammatory activity after topical administration as well as their gastro-intestinal side effects. Several compounds proved to be potent PDE4 inhibitors and some 2-cyanoiminoimidazoles showed less pronounced gastro-intestinal side effects than reference compounds but maintained anti-inflammatory activity after topical administration.