Heterocyclic N-oxides have emerged as potent compounds with anticancer, antibacterial,
antihypertensive, antiparasitic, anti-HIV, anti-inflammatory, herbicidal, neuroprotective, and procognitive
activities. The N-oxide motif has been successfully employed in a number of recent drug development
projects. This review surveys the emergence of this scaffold in the mainstream medicinal
chemistry with a focus on the discovery of the heterocyclic N-oxide drugs, N-oxide-specific mechanisms
of action, drug-receptor interactions and synthetic avenues to these compounds. As the first review
on this subject that covers the developments since 1950s to date, it is expected that it will inspire
wider implementation of the heterocyclic N-oxide motif in the rational design of new medicinal agents.
Keywords: Heterocyclic N-oxides, nitric oxide mimics, bioisosteres, hypoxia, factor Xa inhibitors, coagulation cascade direct
thrombin inhibitors, antichagasic agents, antimalarials.
Rights & PermissionsPrintExport