Bedaquiline
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Bedaquiline
| Bedaquiline | |
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(1R,2S)-1-(6-Bromo-2-methoxy-3-quinolyl)-4-dimethylamino-2-(1-naphthyl)-1-phenyl-butan-2-ol |
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Other names
TMC207; R207910; AIDS222089 |
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| Identifiers | |
| CAS number | 654653-81-3 |
| PubChem | 5746640 |
| ChemSpider | 4534966 |
| UNII | 78846I289Y |
| MeSH | R207910 |
| Jmol-3D images | Image 1 |
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| Properties | |
| Molecular formula | C32H31BrN2O2 |
| Molar mass | 555.5 g mol−1 |
| Except where noted otherwise, data are given for materials in their standard state (at 25 °C, 100 kPa) | |
| Infobox references | |
Bedaquiline (also known as TMC207 or R207910) is an experimental diarylquinoline anti-tuberculosis drug, which was discovered by Koen Andries and his team at Janssen Pharmaceutica.[1] 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,[2] and a trial of 47 patients showed that it is effective in the treatment of M. tuberculosis.[3]
Bedaquiline has been successfully applied in a phase II efficacy study and is being developed by Tibotec and the TB Alliance.[4]
Mode of action
Bedaquiline affects the proton pump for ATP synthase, which is unlike the quinolones, whose target is DNA gyrase.[5]
References
- ^ de Jonge MR, Koymans LH, Guillemont JE, Koul A, Andries K (June 2007). "A computational model of the inhibition of Mycobacterium tuberculosis ATPase by a new drug candidate R207910". Proteins 67 (4): 971–80. doi:10.1002/prot.21376. PMID 17387738.
- ^ Protopopova M, Bogatcheva E, Nikonenko B, Hundert S, Einck L, Nacy CA (May 2007). "In search of new cures for tuberculosis". Med Chem 3 (3): 301–16. doi:10.2174/157340607780620626. PMID 17504204. http://www.sequella.com/docs/TB_Drugs_Review.pdf.
- ^ Diacon AH, Pym A, Grobusch M, Patientia R, Rustomjee R, Page-Shipp L, Pistorius C, Krause R, Bogoshi M, Churchyard G, Venter A, Allen J, Palomino JC, De Marez T, van Heeswijk RP, Lounis N, Meyvisch P, Verbeeck J, Parys W, de Beule K, Andries K, Neeley DF (June 2009). "The Diarylquinoline TMC207 for Multidrug-Resistant Tuberculosis". N. Engl. J. Med. 360 (23): 2397–2405. doi:10.1056/NEJMoa0808427. PMID 19494215.
- ^ Matteelli A, Carvalho AC, Dooley KE, Kritski A (June 2010). "TMC207: the first compound of a new class of potent anti-tuberculosis drugs". Future Microbiol 5 (6): 849–58. doi:10.2217/fmb.10.50. PMC 2921705. PMID 20521931. http://www.pubmedcentral.nih.gov/articlerender.fcgi?tool=pmcentrez&artid=2921705.
- ^ Kotz J (June 2005). "Targeting tuberculosis". Nature Chemical Biology. doi:10.1038/nchembio002.
See also
- Multi-drug-resistant tuberculosis (MDR-TB)
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