Diamino-1,2,4-triazole derivatives are selective inhibitors of TYK2 and JAK1 over JAK2 and JAK3

Tyrosine kinase 2 (TYK2) is required for signaling of interleukin-23 (IL-23), which plays a key role in rheumatoid arthritis. Presented is the design and synthesis of 1,2,4-triazoles, and the evaluation of their inhibitory activity against the Janus associated kinases TYK2 and JAKs 1–3.

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Bibliographische Detailangaben
Veröffentlicht in:	Bioorganic & medicinal chemistry letters 2010-12, Vol.20 (24), p.7454-7457
Hauptverfasser:	Malerich, Jeremiah P., Lam, Jennifer S., Hart, Barry, Fine, Richard M., Klebansky, Boris, Tanga, Mary J., D’Andrea, Annalisa
Format:	Artikel
Sprache:	eng
Schlagworte:	Binding Sites Biological and medical sciences Bones, joints and connective tissue. Antiinflammatory agents Computer Simulation Humans Interleukin-23 - metabolism JAK1 JAK2 JAK3 Janus associated kinase Janus Kinase 1 - antagonists & inhibitors Janus Kinase 1 - metabolism Janus Kinase 2 - antagonists & inhibitors Janus Kinase 2 - metabolism Janus Kinase 3 - antagonists & inhibitors Janus Kinase 3 - metabolism Medical sciences Pharmacology. Drug treatments Protein Kinase Inhibitors - chemical synthesis Protein Kinase Inhibitors - chemistry Protein Kinase Inhibitors - pharmacology Triazoles - chemical synthesis Triazoles - chemistry Triazoles - pharmacology TYK2 TYK2 Kinase - antagonists & inhibitors TYK2 Kinase - metabolism Tyrosine kinase 2
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Beschreibung
Zusammenfassung:	Tyrosine kinase 2 (TYK2) is required for signaling of interleukin-23 (IL-23), which plays a key role in rheumatoid arthritis. Presented is the design and synthesis of 1,2,4-triazoles, and the evaluation of their inhibitory activity against the Janus associated kinases TYK2 and JAKs 1–3.
ISSN:	0960-894X 1464-3405
DOI:	10.1016/j.bmcl.2010.10.026