Novel 1-(2-aminopyrazin-3-yl)methyl-2-thioureas as potent inhibitors of mitogen-activated protein kinase-activated protein kinase 2 (MK-2).

doi:10.1016/j.bmcl.2009.04.088

Paper

DOI: 10.1016/j.bmcl.2009.04.088

Novel 1-(2-aminopyrazin-3-yl)methyl-2-thioureas as potent inhibitors of mitogen-activated protein kinase-activated protein kinase 2 (MK-2).

Published Jun 15, 2009 · Songnian Lin, M. Lombardo, Sunita Malkani

Bioorganic & medicinal chemistry letters

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Abstract

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Novel 1-(2-aminopyrazin-3-yl)methyl-2-thioureas show potent inhibitory activity against MK-2 and suppress TNF expression in THP-1 cells and mice during acute inflammation.

PopulationOlder adults (50-71 years)

Sample size24

MethodsObservational

OutcomesBody Mass Index projections

ResultsSocial networks mitigate obesity in older groups.

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Pyrrolo-pyrimidones: a novel class of MK2 inhibitors with potent cellular activity.

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Synthesis and SAR studies of indole-based MK2 inhibitors.

Indole-based MK2 inhibitors can be improved by introducing aminomethyl groups to lactam rings and expanding the lactam from a 6- to 7-membered ring.

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Pyrazinoindolone inhibitors of MAPKAP-K2 (MK2) provide a balanced balance of cellular potency and physicochemical properties, with MK2 inhibition responsible for sub-micromolar cellular efficacy.

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Chemical Genetics Define the Roles of p38α and p38β in Acute and Chronic Inflammation*

Specific inhibition of the p38 isoform is necessary and sufficient for anti-inflammatory efficacy in vivo.

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Novel tetrahydro-beta-carboline-1-carboxylic acids as inhibitors of mitogen activated protein kinase-activated protein kinase 2 (MK-2).

Novel tetrahydro-beta-carboline-1-carboxylic acids show remarkable selectivity in inhibiting MK-2 and TNFalpha production, offering potential therapeutic applications.

2007·118citations·J. Trujillo et al.·Bioorganic & medicinal chemistry letters

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Novel fluorinated thiourea derivatives show good antibacterial and anticancer activity, particularly fluorinated pyridine derivative 4a, which shows potential as a mitogen activated protein kinase-2 inhibitor.

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DOI: 10.1021/acs.jmedchem.5b01457

Targeting Mitogen-Activated Protein Kinase-Activated Protein Kinase 2 (MAPKAPK2, MK2): Medicinal Chemistry Efforts To Lead Small Molecule Inhibitors to Clinical Trials.

MK2 inhibitors show potential for treating inflammation and related diseases, preventing tumor metastasis, and increasing tumor sensitivity to chemotherapeutics, despite challenges in development.

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