Synthesis and biological evaluation of imidazol-2-one and 2-cyanoiminoimidazole derivatives: novel series of PDE4 inhibitors.

Article Details

Citation

Copy to clipboard

Andres JI, Alonso JM, Diaz A, Fernandez J, Iturrino L, Martinez P, Matesanz E, Freyne EJ, Deroose F, Boeckx G, Petit D, Diels G, Megens A, Somers M, Van Wauwe J, Stoppie P, Cools M, De Clerck F, Peeters D, de Chaffoy D

Synthesis and biological evaluation of imidazol-2-one and 2-cyanoiminoimidazole derivatives: novel series of PDE4 inhibitors.

Bioorg Med Chem Lett. 2002 Feb 25;12(4):653-8.

PubMed ID

11844693 [ View in PubMed

]

Abstract

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.

DrugBank Data that Cites this Article

Binding Properties

Drug	Target	Property	Measurement	pH	Temperature (°C)
(R)-Rolipram	cAMP-specific 3',5'-cyclic phosphodiesterase 4B	IC 50 (nM)	741	N/A	N/A	Details
Piclamilast	cAMP-specific 3',5'-cyclic phosphodiesterase 4B	IC 50 (nM)	0.2	N/A	N/A	Details