Phenylpyridine-2-ylguanidines and rigid mimetics as novel inhibitors of TNF_ overproduction- Beneficial action in models of neuropathic pain and of acute lung
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CNRS, Université de Strasbourg, UMR7200 Laboratoire Innovation Thérapeutique, Illkirch, France

European Journal of Medicinal Chemistry

4-phenylpyridin-2-yl-guanidine (5b): a new inhibitor of the overproduction of pro-inflammatory cytokines (TNF_ and Il1_) was identified from a high-throughput screening of a chemical library on human peripheral blood mononuclear cells (PBMCs) after LPS stimulation. Derivatives, homologues and rigid mimetics of 5b were designed and synthesized, and their cytotoxicity and ability to inhibit TNF_ overproduction were evaluated. Among them, compound 5b and its mimetic 12 (2-aminodihydroquinazoline) showed similar inhibitory activities, and were evaluated in vivo in models of lung inflammation and neuropathic pain in mice. In particular, compound 12 proved to be active (5_mg/kg, ip) in both models.

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