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Isothiazolidinone inhibitors of PTP1B containing imidazoles and imidazolines.

Abstract：

:The structure-based design and synthesis of isothiazolidinone (IZD) inhibitors of PTP1B containing imidazoles and imidazolines and their modification to interact with the B site of PTP1B are described here. The X-ray crystal structures of 3I and 4I complexed with PTP1B were solved and revealed the inhibitors are interacting extensively with the B site of the enzyme.

journal_name

Bioorg Med Chem Lett

journal_title

Bioorganic & medicinal chemistry letters

authors

Douty B,Wayland B,Ala PJ,Bower MJ,Pruitt J,Bostrom L,Wei M,Klabe R,Gonneville L,Wynn R,Burn TC,Liu PC,Combs AP,Yue EW

doi

10.1016/j.bmcl.2007.11.012

subject

Has Abstract

pub_date

2008-01-01 00:00:00

pages

66-71

issue

1

eissn

0960-894X

issn

1464-3405

pii

S0960-894X(07)01322-4

journal_volume

18

pub_type

杂志文章

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