Malerich, J. P., Lam, J. S., Hart, B., Fine, R. M., Klebansky, B., Tanga, M. J., & D’Andrea, A. (2010). Diamino-1, 2, 4-triazole derivatives are selective inhibitors of TYK2 and JAK1 over JAK2 and JAK3. Bioorganic & medicinal chemistry letters, 20(24), 7454-7457.
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.