TMC207 CAS 843663-66-1 Ubunyulu > 99.5% (HPLC)
AbaPhakathi abaNxulumeneyo ne-TMC207:
TMC207 CAS 843663-66-1
I-3-Benzyl-6-Bromo-2-Chloroquinoline CAS 654655-68-2
I-3-Benzyl-6-Bromo-2-Methoxyquinoline CAS 654655-69-3
| Igama leMchiza | TMC207 |
| Izithethantonye | 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 |
| Inombolo yeCAS | 843663-66-1 |
| Inombolo yeCAT | RF2336 |
| Ubume beStokhwe | Kwi-Stock, iMveliso yoMveliso ukuya kwiiToni |
| Ifomula yeemolekyuli | I-C32H31BrN2O2 |
| Ubunzima beMolekyuli | 555.516 |
| Indawo yokunyibilika | 104℃ |
| Ukuxinana | 1.322±0.06 g/cm3 |
| Inovakalelo | Hygroscopic.UkuKhanya okungevayo, ukungeva komoya |
| Uphawu | Ruifu Chemical |
| Into | Iinkcukacha |
| Imbonakalo | Umgubo oMhlophe okanye oMhlophe |
| Ubunyulu / Indlela yokuHlalutya | >99.5% (HPLC) |
| Ilahleko ekomisweni | <0.50% |
| Intsalela kwi-Ignition | <0.20% |
| Nakuphi na Ukungacoceki komntu | <0.10% |
| Isomer | <0.10% |
| Ukungcola ngokupheleleyo | <0.50% |
| Iintsimbi ezinzima (njenge Pb) | <20ppm |
| IArsenic (As) | <2.0ppm |
| I-Infrared Spectrum | Iyahambelana neSakhiwo |
| Proton NMR Spectrum | Iyahambelana neSakhiwo |
| Umgangatho woVavanyo | Umgangatho woShishino |
| Ukusetyenziswa | API |
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(i-CAS: 843663-66-1), (eyaziwa ngokuba yi-TMC207 kunye ne-R207910), ithengiswa phantsi kwegama lokuthengisa i-Sirturo, i-noveli ye-diarylquinoline ye-antimycobacterial drug echaphazela isifo sofuba ngokuvimbela umsebenzi we-M. tuberculosis ATP synthase proton pump.I-ATP synthesis ye-mycobacteria isebenzisa i-antibacterial and bactericidal effects.Ekliniki isetyenziselwa ukunyanga isifo sephepha esinganyangekiyo ngamayeza amaninzi (MDR-PTB).I-TMC207 inomsebenzi ofanayo wokubulala iintsholongwane ngokuchasene nentsholongwane ye-M. yesifo sephepha kunye neentlobo ezixhathisayo, kwaye inesiphumo esihle sokuvala inzala kwiibhaktheriya ezileleyo.NgoDisemba ka-2012, i-FDA yase-US yavuma i-TMC207 njengenxalenye yonyango oludityanisiweyo lonyango lwesifo sephepha esinganyangekiyo ngamachiza amaninzi (MDRTB).I-TMC207 lichiza lokuqala elivunyiweyo le-MDR-TB kwaye liyimvumo yokuqala evela kudidi olutsha lwee-arhente ze-antituberculosis kule minyaka ingama-40 idlulileyo.Ngenxa yesidingo esikhulu esinganyangekiyo sokunyanga i-MDR-TB, i-FDA iye yanika i-TMC207 imvume ekhawulezileyo ngokusekwe kwiziphumo zeSigaba sesi-II, ukunika izigulane ukufikelela kumachiza ngelixa uphononongo olongezelelweyo lwezonyango luqhutywa.I-TMC207 yidayari ye-diarylquinoline eyafunyanwa kubuchule obuphezulu bokuhlola iiseli ezipheleleyo kunye ne-Mycobacterium smegmatis esetyenziswa njenge-surrogate ye-M. tuberculosis.I-TMC207 yi-enantiomer enye ye hit yokuqala yovavanyo.I-TMC207 inomsebenzi onamandla kwaye okhethayo ngokuchasene ne-mycobacteria, kwaye iyasebenza ngokuchasene nesifo sephepha esinguM. esingangeva ngamachiza kunye nesingevani ngamachiza.Indlela yokusebenza ye-TMC207 yohlukile kumachiza achasene ne-TB kwaye ibandakanya uthintelo lwe-mycobacterial ATP synthase;ayisebenzi ngokuchasene ne-ATP synthase yabantu.I-TMC207 inomsebenzi we-vivo kwiimodeli ezininzi zangaphambi kweklinikhi zosulelo lwe-TB, iyodwa kwaye idibene nezinye ii-anti-TB, kwaye inomsebenzi wokubulala iintsholongwane kwiimodeli zosulelo lwe-TB esekiweyo.I-TMC207 yenziwe ngamanyathelo amahlanu ukusuka kwi-3-Phenylpropionic Acid kunye ne-para-Bromoaniline.Ukulandela ukubunjwa kwe-amide, unyango kunye ne-POCl3 kunye ne-DMF phantsi kweemeko ze-Vilsmeier-Hack zinike imveliso ye-2-Chloroquinoline.Unyango nge-sodium methoxide, elandelwa yi-condensation nge-3-(Dimethylamino) -1-(naphthalen-1-yl) propan-1-enye, kunye nokwahlulwa kwe-isomers kunika i-TMC207.
