Imikhiqizo

I-4-(4-Fluorophenyl)-6-isopropyl-2-[(N-methyl-N-methylsulfonyl)amino]pyrimidine-5-yl-methanol, eyaziwa nangokuthi i-Z6, iyinhlanganisela yamakhemikhali enezinhlelo zokusebenza ezingaba khona emkhakheni wezokwelapha. .Isakhiwo sayo esiyingqayizivele namaqembu asebenzayo ayenza ibe ikhandidethi elithakazelisayo lokutholwa nokuthuthukiswa kwezidakamizwa.Okunye okungase kube khona ukusetshenziswa kwe-Z6 njenge-ejenti elwa nokuvuvukala.Ukuvuvukala kudlala indima ezifweni eziningi, okuhlanganisa i-rheumatoid arthritis, isifo samathumbu esivuvukalayo, kanye nesifuba somoya.Iqembu le-phenyl elifakwe esikhundleni se-fluoro esikhundleni se-fluoro kanye ne-pyrimidine core kuyenza ifaneleke ukusebenzisana nemigomo ethile ehilelekile enqubweni yokuvuvukala, okungase kuholele ekwakhiweni kwemithi elwa nokuvuvukala inoveli.I-Z6 nayo inesithembiso njenge-ejenti elwa namagciwane.Ukutheleleka ngegciwane kusalokhu kuwukukhathazeka okubalulekile kwezempilo emhlabeni wonke, futhi kunesidingo esiqhubekayo semithi yokwelapha elwa namagciwane emisha nesebenzayo.Ukuba khona kweqembu le-isopropyl ku-Z6 kuthuthukisa izakhiwo zalo ze-hydrophobic, okulivumela ukuthi likwazi ukungena kulwelwesi lwegciwane futhi luvimbele ukuphindaphinda kwegciwane.Izici zayo zesakhiwo zingathuthukiswa ukuze ziqondise ngokuqondile ama-enzyme noma amaprotheni egciwane, okuholela ekuthuthukisweni kwezidakamizwa ezinamandla ezilwa namagciwane.Ukwengeza, i-Z6 ingase ibe nezinhlelo zokusebenza ekwelapheni umdlavuza.Iqembu le-phenyl elifakwe esikhundleni se-fluoro kanye ne-pyrimidine core ngokuvamile litholakala kumakhompiyutha anomsebenzi wokulwa nomdlavuza.Ngokushintsha ukwakheka kwe-Z6, kungahle kwenzeke ukudala okuphuma kokunye okuqondise kumaseli omdlavuza, kuvimbele ukukhula kwawo futhi kubangele i-apoptosis ngenkathi kulondolozwa amaseli anempilo.Ukunyibilika nokuzinza kwenhlanganisela kungabuye kuthuthukiswe ukuze kuthuthukiswe ukusebenza kahle kwayo futhi kuncishiswe imiphumela engemihle engaba khona.Ngaphezu kwalokho, i-Z6 ingasetshenziswa njengendawo yokuqala yokuhlanganiswa kwemitapo yolwazi yama-molecule noma ama-scaffold amakhemikhali.Inikeza ukuguquguquka kokuguqulwa kanye nokwenza kahle, okuvumela ukuhlolwa kobudlelwane bomsebenzi wesakhiwo kanye nokuhlonzwa kwezinhlanganisela zomthofu ukuze kuthuthukiswe okuqhubekayo.Kafushane, i-Z6 iyinhlanganisela ethembisayo enezinhlelo zokusebenza ezingase zibe khona emkhakheni wezokwelapha.Izici zayo zesakhiwo kanye namaqembu asebenzayo ayenza ifanelekele izinjongo ezihlukahlukene zokwelapha, kuhlanganise nezinhlelo zokulwa nokuvuvukala, i-antiviral, kanye ne-anti-cancer.Ngocwaningo olwengeziwe nokuthuthukiswa, i-Z6 kanye nokuphuma kwayo kunamandla okwenza igalelo elibalulekile ekutholweni kwezidakamizwa futhi kube neqhaza ekuthuthukisweni kwezindlela zokwelapha ezinoveli nezisebenzayo.