Lihlahisoa

(+)-(3R,5S), tert-Butyl 7-[4-(4-fluorophenyl)-6-isopropyl-2-(N-methyl-N-methylsulphonylamino)-pyrimidin-5-yl]-3,5 -dihydroxy-6(E) -heptenate, e tsejoang hape e le R1.5 kapa tert-butyl-rosuvastatin, ke motsoako oa lik'hemik'hale o nang le lisebelisoa tse ka sebelisoang indastering ea meriana.Rosuvastatin ke meriana e tsebahalang ea ho theola k'holeseterole e leng ea sehlopha. lithethefatsi tse bitsoang li-statins.E sebetsa ka ho thibela enzyme e bitsoang HMG-CoA reductase, e amehang tlhahisong ea k'holeseterole 'meleng.R1.5 ke derivative ea rosuvastatin e nang le sehlopha sa tert-butyl se kopantsoeng le molek'hule, se fanang ka thepa e eketsehileng le melemo e ka 'nang ea e-ba teng.E 'ngoe e ka sebelisoang ea R1.5 ke motsoako oa meriana bakeng sa phekolo ea hyperlipidemia le thibelo ea mafu a pelo.Joalo ka rosuvastatin, R1.5 e ka sebelisoa ho theola maemo a cholesterol ea LDL, e tsejoang hape e le "cholesterol" e mpe, le triglycerides maling.Motsoako ona o ka bonts'a thepa e ntlafalitsoeng ea pharmacokinetic, joalo ka ho eketseha ha bioavailability kapa botsitso bo ntlafetseng, ha bo bapisoa le lithethefatsi tsa motsoali.Ho feta moo, sehlopha sa tert-butyl se ka kenya letsoho ho qhibiliheng ha motsoako le ho hlahisa mekhoa e mengata, ho etsa hore e tšoanele mekhoa e fapaneng ea ho fana ka lithethefatsi. Tšebeliso e 'ngoe e ka bang teng ea R1.5 ke ho nts'etsopele ea lihlahisoa kapa mekhoa e lebisitsoeng ea ho fana ka lithethefatsi.Sehlopha sa tert-butyl se ka sebetsa e le sehlopha se sireletsang, se lumellang tokollo e laoloang ea rosuvastatin ka har'a lisele kapa litho tse itseng, joalo ka sebete.Leano lena le ka ntlafatsa katleho ea moriana le ho fokotsa litla-morao tse ka 'nang tsa e-ba teng ka ho eketsa mahloriso a eona sebakeng se lebeletsoeng ha ho ntse ho fokotsa ho pepeseha ha lisele tse sa lebelloang.Ho phaella moo, R1.5 e ka sebetsa e le sesebelisoa sa bohlokoa bakeng sa litsebi tsa meriana ea meriana ho sibolloang le nts'etsopele ea lithethefatsi.Sebopeho se rarahaneng sa motsoako se fana ka sethala bakeng sa liphetoho tse ling le tse ling.Bafuputsi ba ka sebelisa R1.5 e le motsoako o etellang pele ho lekola likamano tsa ts'ebetso le ts'ebetso le ho nts'etsapele li-analogue tse ncha tse nang le potency e ntlafalitsoeng, khetho, kapa lintlha tse ntlafalitsoeng tsa kalafo.Lithuto tse joalo li ka kenya letsoho ho nts'etsopele ea li-statins tse ncha le tse sebetsang haholoanyane kapa li-agent tse ling tse theolang k'holeseterole. Qetellong, (+) - (3R,5S), tert-Butyl 7-[4- (4-fluorophenyl) -6-isopropyl -2-(N-methyl-N-methylsulphonylamino)-pyrimidin-5-yl]-3,5-dihydroxy-6(E) -heptenate (R1.5 kapa tert-butyl-rosuvastatin) e na le tšepiso e le motsoako oa meriana bakeng sa kalafo ea hyperlipidemia le mafu a pelo.Sebopeho sa eona se ikhethang, se kopantsoeng le sehlopha sa tert-butyl, se ka fana ka melemo e kang pharmacokinetics e ntlafetseng, phano ea lithethefatsi e lebisitsoeng, le menyetla ea ntlafatso e eketsehileng ea lithethefatsi.Lipatlisiso tse ling le nts'etsopele lia hlokahala ho hlahloba ka botlalo bokhoni ba R1.5 lefapheng la meriana.