R207910

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ImageFile=R207910.svg
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IUPACName=(1R,2R)-1-(6-bromo-2-methoxyquinolin-3-yl)- 4-(dimethylamino)-2-(3-fluorophenyl)-1-phenylbutan-2-ol
OtherNames=AIDS222089
Section1= Chembox Identifiers
CASNo=654653-81-3
PubChem=5746640
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MeSHName=R207910
Section2= Chembox Properties
Formula=C₂₈H₂₈BrFN₂O₂
MolarMass=523.437 g/mol
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R207910 (also known as TMC207) is an experimental diarylquinoline anti-tuberculosis drug, which was discovered by Koen Andries and his team at Janssen Pharmaceutica [Andries K, Verhasselt P, Guillemont J, et al. (2005), A diarylquinoline drug active on the ATP-synthase of Mycobacterium tuberculosis, Science 307 (5707): 223–27] [cite journal |author=de Jonge MR, Koymans LH, Guillemont JE, Koul A, Andries K |title=A computational model of the inhibition of Mycobacterium tuberculosis ATPase by a new drug candidate R207910 |journal=Proteins |volume=67 |issue=4 |pages=971–80 |year=2007 |pmid=17387738 |doi=10.1002/prot.21376] . It was described for the first time in 2004 at the Interscience Conference on Antimicrobial Agents and Chemotherapy (ICAAC) meeting Late-Breaker Session, after the drug had been in development for over 7 years [ [http://www.sequella.com/docs/TB_Drugs_Review.pdf In Search of New Cures for Tuberculosis] ] .

Mode Of Action

R207910 affects the proton pump for ATP synthase, which is unlike other quinolones, whose target is DNA gyrase. [ [http://www.nature.com/nchembio/journal/vaop/nprelaunch/full/nchembio002.html Joanne Kotz, Targeting tuberculosis, Nature Chemical Biology, Published online: 8 February 2005] (doi: 10.1038/nchembio002)]

References

ee also

* Multi-drug-resistant tuberculosis (MDR-TB)