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Current Medicinal Chemistry

Editor-in-Chief

ISSN (Print): 0929-8673
ISSN (Online): 1875-533X

Heterocyclic N-Oxides - An Emerging Class of Therapeutic Agents

Author(s): A.M. Mfuh and O.V. Larionov

Volume 22, Issue 24, 2015

Page: [2819 - 2857] Pages: 39

DOI: 10.2174/0929867322666150619104007

Price: $65

Abstract

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.


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