Imikhiqizo

(+)-(3R,5S), tert-Butyl 7-[4-(4-fluorophenyl)-6-isopropyl-2-(N-methyl-N-methylsulphonylamino)-pyrimidin-5-yl]-3,5 -dihydroxy-6(E) -heptenate, eyaziwa nangokuthi i-R1.5 noma i-tert-butyl-rosuvastatin, iyinhlanganisela yamakhemikhali engase isetshenziswe embonini yezemithi.I-Rosuvastatin umuthi owaziwa kakhulu wokwehlisa i-cholesterol oseklasini. izidakamizwa ezibizwa ngokuthi ama-statins.Isebenza ngokuvimbela i-enzyme ebizwa ngokuthi i-HMG-CoA reductase, ebandakanyeka ekukhiqizeni i-cholesterol emzimbeni.I-R1.5 iwukuphuma kwe-rosuvastatin equkethe iqembu le-tert-butyl elinamathiselwe ku-molecule, ehlinzeka ngezakhiwo ezengeziwe kanye nezinzuzo ezingaba khona.Okunye okungenzeka ukuthi kusetshenziswe u-R1.5 njengesithako sokwenza imithi yokwelapha i-hyperlipidemia kanye nokuvimbela izifo zenhliziyo nemithambo yegazi.Njenge-rosuvastatin, i-R1.5 ingasetshenziswa ukwehlisa amazinga e-LDL cholesterol, eyaziwa nangokuthi "i-cholesterol" embi, kanye ne-triglycerides egazini.Le nhlanganisela ingase ibonise izakhiwo ze-pharmacokinetic ezithuthukisiwe, ezifana nokukhuphuka kwe-bioavailability noma ukuqina okuthuthukisiwe, uma kuqhathaniswa nomuthi ongumzali.Ngaphezu kwalokho, iqembu le-tert-butyl lingase libe negalelo ekuncibilikeni nasekukhiqizeni izinto ezihlukahlukene, okulenze lifanelekele izinhlelo ezihlukahlukene zokulethwa kwezidakamizwa. Okunye okungase kusetshenziswe u-R1.5 ukwakhiwa kwezidakamizwa noma amasistimu okulethwa kwezidakamizwa okuhlosiwe.Iqembu le-tert-butyl lingasebenza njengeqembu elivikelayo, elivumela ukukhululwa okulawulwayo kwe-rosuvastatin ezicutshini noma ezithweni ezithile, njengesibindi.Leli su lingathuthukisa ukusebenza komuthi futhi linciphise imiphumela engemihle engaba khona ngokukhulisa ukugxila kwawo endaweni okuqondiswe kuyo kuyilapho kunciphisa ukuchayeka ezicutshini ezingahlosiwe. Ngaphezu kwalokho, u-R1.5 ungasebenza njengethuluzi elibalulekile losokhemisi bezokwelapha ekutholakaleni nasekuthuthukisweni kwezidakamizwa.Isakhiwo esiyinkimbinkimbi se-compound sinikeza inkundla yezinye izinguquko kanye nokuphuma kokunye.Abacwaningi bangasebenzisa u-R1.5 njengenhlanganisela eholayo ukuhlola ubudlelwano bomsebenzi wesakhiwo futhi bathuthukise ama-analog amasha anamandla athuthukisiwe, ukukhetha, noma amaphrofayili athuthukisiwe okwelapha.Ucwaningo olunjalo lungase lube nomthelela ekwakhiweni kwenoveli kanye nama-statins asebenza kangcono noma amanye ama-agent anciphisa i-cholesterol. Ekugcineni, (+)-(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 noma i-tert-butyl-rosuvastatin) inesithembiso njengenhlanganisela yemithi ukwelashwa kwe-hyperlipidemia kanye nezifo zenhliziyo.Isakhiwo sayo esiyingqayizivele, esihlanganiswe neqembu le-tert-butyl, singanikeza izinzuzo ezifana ne-pharmacokinetics ethuthukisiwe, ukulethwa kwezidakamizwa okuhlosiwe, kanye namathuba okuqhubeka nokuthuthukiswa kwezidakamizwa.Kudingeka olunye ucwaningo nentuthuko ukuze kuhlolwe ngokugcwele amandla angama-R1.5 emkhakheni wezokwenziwa kwemithi.