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Article Dans Une Revue Bioorganic and Medicinal Chemistry Letters Année : 2011

Synthesis and evaluation of thiophenyl derivatives as inhibitors of alkaline phosphatase

Résumé

Pathological calcifications induced by deposition of basic phosphate crystals or hydroxyapatite (HA) on soft tissues are a large family of diseases comprising of ankylosing spondylitis (AS), end-stage osteoarthritis (OA) and vascular calcification. High activity of tissue non-specific alkaline phosphatase (TNAP) is a hallmark of pathological calcifications induced by HA deposition. The use of TNAP inhibitor is a possible therapeutic option to address calcific diseases produced by HA deposition on soft tissues. We report the synthesis of a series of thiopheno-imidazo[2,1-b]thiazole derivatives which were evaluated as potential inhibitors of TNAP displaying a large range of IC50 at pH 10.4 (from 42 ± 13 μM to more than 800 μM).

Dates et versions

hal-00692020 , version 1 (27-04-2012)

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L. Chang, D. Le Duy, S. Mébarek, F. Popowycz, S Pellet-Rostaing, et al.. Synthesis and evaluation of thiophenyl derivatives as inhibitors of alkaline phosphatase. Bioorganic and Medicinal Chemistry Letters, 2011, 21 (8), pp.2297-2301. ⟨10.1016/j.bmcl.2011.02.089⟩. ⟨hal-00692020⟩
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