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]
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