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

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 Lett

authors

Chang L,Duy do L,Mébarek S,Popowycz F,Pellet-Rostaing S,Lemaire M,Buchet R

doi

10.1016/j.bmcl.2011.02.089

subject

Has Abstract

pub_date

2011-04-15 00:00:00

pages

2297-301

issue

8

eissn

0960-894X

issn

1464-3405

pii

S0960-894X(11)00273-3

journal_volume

21

pub_type

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