R207910
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R207910 | |
---|---|
IUPAC name | (1R,2R)-1-(6-bromo-2-methoxyquinolin-3-yl)- 4-(dimethylamino)-2-
(3-fluorophenyl)-1-phenylbutan-2-ol |
Other names | AIDS222089 |
Identifiers | |
CAS number | [654653-81-3] |
PubChem | |
MeSH | |
Properties | |
Molecular formula | C28H28BrFN2O2 |
Molar mass | 523.437 g/mol |
Except where noted otherwise, data are given for materials in their standard state (at 25 °C, 100 kPa) Infobox disclaimer and references |
R207910 (also known as TMC207) is an experimental diarylquinoline anti-tuberculosis drug, which was discovered by Koen Andries and his team at Janssen Pharmaceutica[1][2]. 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[3].
[edit] Mode Of Action
R207910 affects the proton pump for ATP synthase, which is unlike other quinolones, whose target is DNA gyrase.[4]
[edit] References
- ^ 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
- ^ de Jonge MR, Koymans LH, Guillemont JE, Koul A, Andries K (2007). "A computational model of the inhibition of Mycobacterium tuberculosis ATPase by a new drug candidate R207910". Proteins 67 (4): 971–80. doi: . PMID 17387738.
- ^ In Search of New Cures for Tuberculosis
- ^ Joanne Kotz, Targeting tuberculosis, Nature Chemical Biology, Published online: 8 February 2005 (doi: 10.1038/nchembio002)
[edit] See also
- Multi-drug-resistant tuberculosis (MDR-TB)