dc.contributor.author |
Denny, William |
en |
dc.contributor.author |
Palmer, Brian |
en |
dc.coverage.spatial |
England |
en |
dc.date.accessioned |
2011-11-18T02:09:20Z |
en |
dc.date.issued |
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 |
http://hdl.handle.net/2292/9377 |
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
http://www.sherpa.ac.uk/romeo/issn/1756-8919/ |
en |
dc.rights.uri |
https://researchspace.auckland.ac.nz/docs/uoa-docs/rights.htm |
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 |
http://purl.org/eprint/accessRights/RestrictedAccess |
en |
pubs.subtype |
Review |
en |
pubs.elements-id |
150563 |
en |
pubs.org-id |
Medical and Health Sciences |
en |
pubs.org-id |
Medical Sciences |
en |
pubs.org-id |
Auckland Cancer Research |
en |
pubs.org-id |
Science |
en |
pubs.org-id |
Science Research |
en |
pubs.org-id |
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 |