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Issue 4, 2011
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Conformational effects on potency of thioimidazoles and dihydrothiazolines

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Abstract

We investigated the effect of steric restriction and hindrance on inhibitors directed against the biological activity of p38α MAP kinase. The structural reduction of the early lead compound SKF86002 into three structural classes of optimized SKF86002-like inhibitors produced a strong effect on inhibitory potency. This effect was investigated by conformational analysis and docking experiments.

Graphical abstract: Conformational effects on potency of thioimidazoles and dihydrothiazolines

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Publication details

The article was received on 19 Nov 2010, accepted on 05 Jan 2011 and first published on 27 Jan 2011


Article type: Concise Article
DOI: 10.1039/C0MD00228C
Med. Chem. Commun., 2011,2, 261-269

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    Conformational effects on potency of thioimidazoles and dihydrothiazolines

    R. Selig, V. Schattel, M. Goettert, D. Schollmeyer, W. Albrecht and S. Laufer, Med. Chem. Commun., 2011, 2, 261
    DOI: 10.1039/C0MD00228C

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