I-Clenbuterol, iyi-agonist ye-β2-adrenergic (i-agonist ye-β2-adrenergic), efana ne-ephedrine (i-Ephedrine), ivame ukusetshenziswa emtholampilo ukwelapha isifo samaphaphu esingamahlalakhona (i-COPD). Iphinde isetshenziswe njenge-bronchodilator ukuze kuncishiswe ukubhebhetheka okukhulu kwe-asthma. Ekuqaleni kwawo-1980, inkampani yaseMelika i-Cyanamid yathola ngephutha ukuthi inemiphumela esobala yokukhuthaza ukukhula, ukuthuthukisa izinga lenyama engenamafutha kanye nokunciphisa amafutha, ngakho-ke yasetshenziswa njenge-clenbuterol ekukhuliseni izilwane. Kodwa-ke, ngenxa yemiphumela yayo emibi, i-European Community yavimbela ukusetshenziswa kwe-clenbuterol njengesithako sokudla kusukela ngoJanuwari 1, 1988. Yavinjelwa yi-FDA ngo-1991. Ngo-1997, uMnyango Wezolimo weRiphabhulikhi Yabantu baseShayina wavimbela ngokuqinile ukusetshenziswa kwama-hormone e-beta-adrenergic ekukhiqizeni ukudla kanye nokufuya izilwane, kanti i-Clenbuterol hydrochloride yabekwa endaweni yokuqala.
Kodwa-ke, i-Clenbuterol ye-racemic isanda kuboniswa ukuthi inciphisa ingozi yesifo sikaParkinson. Ukuze kuqinisekiswe ukuthi yiziphi (noma zombili) ama-isomers akhiqiza lo mphumela, i-enantiomer ye-Clenbuterol emsulwa idinga ukufundwa ngokwehlukana.
Esihlokweni sakamuva, iqembu locwaningo lika-Elisabeth Egholm Jacobsen woMnyango WezeKhemistri, eNyuvesi Yesayensi Nobuchwepheshe yaseNorway, ngokubambisana noDkt. Zhu Wei waseShangke Bio, likhuthaze ukwenziwa kwe-ketoreductase KRED kanye ne-cofactor nicotinamide adenine dinucleoside phosphate (NADPH). (R)-1-(4-Amino-3,5-dichlorophenyl)-2-bromoethan-1-ol, ee > 93%; kanye ne-(S)-N-(2 yakhiwe ngohlelo olufanayo ,6-Dichloro-4-(1-hydroxyethyl)phenyl)acetamide, ee >98%. Zombili lezi zinto eziphakathi ezingenhla ziyizinto ezingaba khona ezandulela ama-isomers e-clenbuterol. I-ketoreductase ES-KRED-228 esetshenziswe kulolu cwaningo yayivela eShangke Biopharmaceutical (Shanghai) Co., Ltd. Umphumela wocwaningo othi "Chemoenzymatic Synthesis of Synthons as Precursors for Enantiopure Clenbuterol and Other -2-Agonists" wanyatheliswa ku-"Catalysts" ngoNovemba 4, 2018.
Isikhathi sokuthunyelwe: Agasti-26-2022