5029-05-0Relevant academic research and scientific papers
Synthesis and evaluation of thiophenyl derivatives as inhibitors of alkaline phosphatase
Chang, Lei,Duy, Do Le,Mébarek, Saida,Popowycz, Florence,Pellet-Rostaing, Stéphane,Lemaire, Marc,Buchet, René
supporting information; experimental part, p. 2297 - 2301 (2011/05/15)
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).
