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Synthesis and evaluation of thiophenyl derivatives as inhibitors of alkaline phosphatase.

Bioorganic & medicinal chemistry letters (2011-03-23)
Lei Chang, Do Le Duy, Saida Mébarek, Florence Popowycz, Stéphane Pellet-Rostaing, Marc Lemaire, René Buchet
ABSTRACT

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 IC(50) at pH 10.4 (from 42±13 μM to more than 800 μM).

MATERIALS
Product Number
Brand
Product Description

Sigma-Aldrich
(−)-Tetramisole hydrochloride, ≥99% (GC)
Supelco
Levamisol hydrochloride, VETRANAL®, analytical standard