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).
journal_name
Bioorg Med Chem Lettjournal_title
Bioorganic & medicinal chemistry lettersauthors
Chang L,Duy do L,Mébarek S,Popowycz F,Pellet-Rostaing S,Lemaire M,Buchet Rdoi
10.1016/j.bmcl.2011.02.089subject
Has Abstractpub_date
2011-04-15 00:00:00pages
2297-301issue
8eissn
0960-894Xissn
1464-3405pii
S0960-894X(11)00273-3journal_volume
21pub_type
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