Benzothiazole based inhibitors of p38alpha MAP kinase.

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Liu C, Lin J, Pitt S, Zhang RF, Sack JS, Kiefer SE, Kish K, Doweyko AM, Zhang H, Marathe PH, Trzaskos J, Mckinnon M, Dodd JH, Barrish JC, Schieven GL, Leftheris K

Benzothiazole based inhibitors of p38alpha MAP kinase.

Bioorg Med Chem Lett. 2008 Mar 15;18(6):1874-9. doi: 10.1016/j.bmcl.2008.02.011. Epub 2008 Feb 10.

PubMed ID
18296051 [ View in PubMed
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Abstract

Rational design, synthesis, and SAR studies of a novel class of benzothiazole based inhibitors of p38alpha MAP kinase are described. The issue of metabolic instability associated with vicinal phenyl, benzo[d]thiazol-6-yl oxazoles/imidazoles was addressed by the replacement of the central oxazole or imidazole ring with an aminopyrazole system. The proposed binding mode of this new class of p38alpha inhibitors was confirmed by X-ray crystallographic studies of a representative inhibitor (6a) bound to the p38alpha enzyme.

DrugBank Data that Cites this Article

Binding Properties
DrugTargetPropertyMeasurementpHTemperature (°C)
6-[4-(2-fluorophenyl)-1,3-oxazol-5-yl]-N-(1-methylethyl)-1,3-benzothiazol-2-amineMitogen-activated protein kinase 14IC 50 (nM)6.4N/AN/ADetails