| Literature DB >> 15662951 |
Nicolas Gouault1, Benoit Pinel, Jean-Francois Cupif, Alexandra Depince, Corinne A E Martin-Chouly, Chantal Belleguic, Michele David.
Abstract
A solid-phase route for the preparation of 4a,5,8,8a-tetrahydrophthalazinon-1-ones employing the Diels-Alder reaction has been developed. Some of the new compounds have been tested for inhibition of LPS-stimulated TNF-alpha production in human whole blood from patients with chronic obstructive pulmonary disease (COPD). This evaluation revealed two compounds 17 and 18 of interest, incorporating an arylpiperazine moiety, which were found to inhibit LPS-induced TNF-alpha release like the well known anti-inflammatory PDE4 inhibitors, rolipram and roflumilast.Entities:
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Year: 2004 PMID： 15662951 DOI： 10.1080/14756360412331280536
Source DB: PubMed Journal: J Enzyme Inhib Med Chem ISSN： 1475-6366 Impact factor: 5.051