TMC207 CAS 843663-66-1 Maʻemaʻe >99.5% (HPLC)
| Inoa Kimia | TMC207 |
| Nā huaʻōlelo like | TMC-207, R207910;Sirturo;(αS,βR)-6-Bromo-α-[2-(dimethylamino)ethyl]-2-methoxy-α-1-naphthalenyl-β-phenyl-3-Quinolineethanol;1-(6-Bromo-2-methoxyquinolin-3-yl)-4-dimethylamino-1-phenyl-2-(1-naphthyl) 2-butanol |
| Helu CAS | 843663-66-1 |
| Helu CAT | RF2336 |
| Kūlana Kūʻai | Ma ka waihona, hoʻonui ʻia a hiki i nā tona |
| ʻĀpana Molekala | C32H31BrN2O2 |
| Kaumaha Molecular | 555.516 |
| Lae hehee | 104 ℃ |
| ʻO ka mānoanoa | 1.322±0.06 g/cm3 |
| Pilikino | Hygroscopic.Māmā Māmā, ʻEa Ea |
| Brand | Kemika Ruifu |
| 'ikamu | Nā kikoʻī |
| Ka nana aku | Pada keʻokeʻo a i ʻole keʻokeʻo |
| Maʻemaʻe / Kaʻina Hanana | >99.5% (HPLC) |
| Nalo ma ka maloo | <0.50% |
| Koena ma ka Ignition | <0.20% |
| ʻO kēlā me kēia haumia kanaka | <0.10% |
| Isomer | <0.10% |
| Huina paumaele | <0.50% |
| Nā Metala Kaumaha (e like me Pb) | <20ppm |
| Arsenic (As) | <2.0ppm |
| Infrared Spectrum | Kūlike i ka hoʻolālā |
| Proton NMR Spectrum | Kūlike i ka hoʻolālā |
| Kūlana hoʻāʻo | Kūlana ʻoihana |
| Hoʻohana | API |
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(CAS: 843663-66-1), (ʻike ʻia ʻo TMC207 a me R207910), kūʻai ʻia ma lalo o ka inoa kalepa ʻo Sirturo, he lāʻau lapaʻau diarylquinoline antimycobacterial novel e pili ana i ka maʻi maʻi ma ke kāohi ʻana i ka hana o ka M. tuberculosis ATP synthase proton pump.Hoʻokomo ka ATP synthesis o ka mycobacteria i ka hopena antibacterial a me ka bactericidal.Hoʻohana ʻia i ka maʻi maʻi no ka mālama ʻana i ka maʻi maʻi maʻi multidrug-resistant (MDR-PTB).Loaʻa i ka TMC207 ka hana bactericidal like me ka M. tuberculosis sensitive strains a me ke kū'ē kū'ē, a he maikaʻi hoʻi ka hopena sterilization ma luna o nā bacteria dormant.I Kekemapa 2012, ua ʻae ka US FDA i ka TMC207 ma ke ʻano he ʻāpana o ka lāʻau hoʻohui no ka mālama ʻana i ka maʻi maʻi maʻi kūʻokoʻa-lāʻau (MDRTB).ʻO TMC207 ka lāʻau lapaʻau mua i ʻae ʻia no ka MDR-TB a ʻo ia ka ʻae mua ʻia mai kahi papa hou o nā mea antituberculosis i nā makahiki he 40 i hala.Ma muli o ke kiʻekiʻe o ka pono no ka mālama ʻana i ka MDR-TB, ua hāʻawi ka FDA i ka ʻae wikiwiki ʻana iā TMC207 e pili ana i nā hopena o ka Phase II, e hāʻawi ana i nā mea maʻi i ke komo ʻana i ka lāʻau i ka wā e hana ʻia ana nā haʻawina hauʻoli hou.ʻO TMC207 kahi diarylquinoline i ʻike ʻia mai kahi kiʻekiʻe-throughput, holoʻokoʻa-cell screening plan me Mycobacterium smegmatis i hoʻohana ʻia ma ke ʻano he pani no M. tuberculosis.ʻO TMC207 kahi enantiomer hoʻokahi o kahi hōʻike hōʻike mua.He hana ikaika ko TMC207 e kū'ē i ka mycobacteria, a he ikaika ia e kū'ē i ka M. tuberculosis pili i ka lāʻau a me ka lāʻau.ʻO ke ʻano o ka hana a TMC207 he kū hoʻokahi i waena o nā lāʻau anti-TB a pili i ka pale ʻana i ka mycobacterial ATP synthase;ʻAʻole ia e kūʻē i ka synthase ATP kanaka.Loaʻa iā TMC207 ka hana in vivo i nā ʻano hoʻohālike preclinical o ka maʻi TB, hoʻokahi wale nō a hui pū me nā lāʻau anti-TB ʻē aʻe, a he hana bactericidal i nā ʻano maʻi TB i hoʻokumu ʻia.Hoʻohui ʻia ʻo TMC207 i ʻelima mau ʻanuʻu mai ka 3-Phenylpropionic Acid a me ka para-Bromoaniline.Ma hope o ka hoʻokumu ʻana o ka amide, mālama ʻia me POCl3 a me DMF ma lalo o nā kūlana Vilsmeier-Hack i hāʻawi i kahi huahana 2-Chloroquinoline.Hoʻomaʻamaʻa me ka sodium methoxide, a ukali ʻia e ka condensation me 3-(Dimethylamino) -1-(naphthalen-1-yl) propan-1-one, a me ka hoʻokaʻawale ʻana o nā isomers i hāʻawi iā TMC207.
