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The pyrazine unit is an important structural motif that widely existed in many bioactive and nature compounds.[1] Pyrazine derivatives have attracted wide pharmaceutical interests because of their potential uses in the treatment of psychiatric disorders, neurological diseases (e.g., stress, anxiety and depression), and cardiovascular disorders.[2] They are reported to modulate the activity of CRF1 (corticotropin-releasing factor 1) receptors. Besides, they are also versatile building blocks in the synthesis of VCAM-1 (vascular cell adhesion molecule-1) inhibitors, pyrazine alkaloids (antineoplasmic activity), and imidazopyrazin coelenterazine (bioluminescent). [2] In recent years, pyrazine scaffold has been found in more and more drug molecules.[3-7]
[1] Advanced Synthesis & Catalysis (2020), 362(17), 3621-3626.
[2] Tetrahedron Letters (2009), 50(14), 1618-1621.
[3] Journal of Medicinal Chemistry (2020), Ahead of Print.DOI: 10.1021/acs.jmedchem.0c01170
[4] Journal of Medicinal Chemistry (2015), 58(17), 6753-6765.
[5] Journal of Medicinal Chemistry (2015), 58(13), 5344-5354.
[6] Journal of Medicinal Chemistry (2018), 61(5), 1821-1832.
[7] Journal of Medicinal Chemistry (2018), 61(13), 5525-5546.
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