The nitroimidazooxazines (PA-824 and analogs): structure-activity relationship and mechanistic studies.

Show simple item record Denny, William en Palmer, Brian en
dc.coverage.spatial England en 2011-11-18T02:09:20Z en 2010-08 en
dc.identifier.citation Future Medicinal Chemistry 2(8):1295-1304 Aug 2010 en
dc.identifier.issn 1756-8919 en
dc.identifier.uri en
dc.description.abstract PA-824 is an experimental anti-tubercular agent that has a novel mechanism of action. It is effective against both active and persistent forms of the disease and has recently shown early bactericidal activity in a Phase II clinical trial. This review summarizes recent studies on the mode of action of PA-824 and outlines successful efforts to prepare more effective second-generation analogs. PA-824 displays unusual chemistry following both enzymatic and radiolytic reduction, which is clearly related to its activity as an anti-tubercular agent. The nitroreductase enzyme deazaflavin-dependent nitroreductase, reduces PA-824 with loss of the nitro group, generating reactive nitrogen species such as nitric oxide, which appear important in mediating the activity of the drug. Bioreductive drugs such as PA-824 hold the promise of shorter treatment regimens. en
dc.language eng en
dc.publisher Future Science en
dc.relation.ispartofseries Future Medicinal Chemistry en
dc.rights Items in ResearchSpace are protected by copyright, with all rights reserved, unless otherwise indicated. Previously published items are made available in accordance with the copyright policy of the publisher. Details obtained from en
dc.rights.uri en
dc.subject Animals en
dc.subject Antitubercular Agents en
dc.subject Humans en
dc.subject Mycobacterium tuberculosis en
dc.subject Nitroimidazoles en
dc.subject Structure-Activity Relationship en
dc.subject Tuberculosis en
dc.title The nitroimidazooxazines (PA-824 and analogs): structure-activity relationship and mechanistic studies. en
dc.type Journal Article en
dc.identifier.doi 10.4155/FMC.10.207 en
pubs.issue 8 en
pubs.begin-page 1295 en
pubs.volume 2 en
dc.rights.holder Copyright: FUTURE SCI LTD en
dc.identifier.pmid 21426020 en
pubs.end-page 1304 en
dc.rights.accessrights en
pubs.subtype Review en
pubs.elements-id 150563 en Medical and Health Sciences en Medical Sciences en Auckland Cancer Research en Science en Science Research en Maurice Wilkins Centre (2010-2014) en
dc.identifier.eissn 1756-8927 en
pubs.record-created-at-source-date 2011-11-18 en
pubs.dimensions-id 21426020 en

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