In last decade, the development of new drugs and drug products for central nervous system (CNS)
has remained limited due to incomplete elucidation of pathophysiology of many CNS disorders, complexity
of the diseases and the lack of technologies for delivery through the blood-brain barrier (BBB). In this article
we will summarize the development of diazenyl derivatives of many biologically active moieties like benzodiazepine,
formazan, indole, pyrimidine, thiazole, sulfonamide etc. as diagnostic and therapeutic agents for
CNS. The potential of already existing azo compounds as potent CNS agents have also been discussed. This
overview will provide the researchers an opportunity for further development of new diazenyl derivatives in CNS area.