Imikhiqizo

I-Tert-butyl 4-(6-((6-(1-butoxyvinyl)-8-cyclopentyl-5-methyl-7-oxo-7,8-dihydropyrido[2,3-d]pyrimidin-2-yl)amino) I-pyridin-3-yl)piperazine-1-carboxylate iyinhlanganisela enamandla amakhulu kukhemikhali yezokwelapha kanye nokuthuthukiswa kwezidakamizwa.Isakhiwo sayo samangqamuzana esiyinkimbinkimbi siphakamisa izinhlobonhlobo zezicelo ezingase zibe khona.Le nhlanganisela iqukethe i-piperazine-1-carboxylate core, okuyi-scaffold esetshenziswa kakhulu kukhemikhali yezokwelapha ngenxa yemvelo yayo eguquguqukayo kanye nohlu olubanzi lwamathuba okuhloswe kwezidakamizwa.Ukuba khona kwe-piperazine moiety kuvumela ukusebenzisana nama-receptors ahlukahlukene kanye nama-enzyme, okwenza kube ikhandidethi elithakazelisayo lokuthuthukiswa kwama-agent okwelapha.I-6-(1-butoxyvinyl) -8-cyclopentyl-5-methyl-7-oxo-7, Iqembu le-8-dihydropyrido[2,3-d]pyrimidin-2-yl esakhiweni linikeza umsebenzi ongase ube khona we-pharmacological.Imikhiqizo enjalo ye-pyrido[2,3-d]pyrimidine iye yacutshungulwa kabanzi ngezindawo zayo zokulwa nokuvuvukala, i-antiviral, kanye ne-anti-cancer.Amaqembu e-cyclopenyl kanye ne-methyl afaka isandla ekwenzeni i-lipophilicity ye-compound, engathuthukisa ukufinyeleleka kwayo kwamaselula kanye ne-bioavailability.Iqembu le-tert-butyl ester linikeza ukuzinza ku-compound futhi lingaguqulelwa kalula kwamanye amaqembu asebenzayo, okuvumela ukuguqulwa okuqhubekayo noma ukukhishwa.Lokhu kuguquguquka kubalulekile kumakhemikhali emithi, njengoba kwenza ukuthuthukiswa kwamakhemikhali anamandla futhi akhethiwe.Iqembu le-pyridin-3-yl esakhiweni lisebenza njenge-ligand engaba khona yama-receptors ahlukahlukene, njenge-G protein-coupled receptors (GPCRs).Lokhu kuphakamisa ukuthi i-compound ingaba nomthelela ezindleleni zokubonisa izimpawu ze-intracellular futhi ingabuye ihlolwe amandla ayo njenge-modulator noma umphikisi wama-receptors athile ahilelekile ezimweni zesifo.Isakhiwo sonke se-tert-butyl 4-(6-((6-) (1-butoxyvinyl)-8-cyclopentyl-5-methyl-7-oxo-7,8-dihydropyrido[2,3-d]pyrimidin-2-yl)amino)pyridin-3-yl)piperazine-1-carboxylate avelele amandla ayo ekuthuthukisweni kwezindlela zokwelapha ezinoveli.Inikeza amathuba okuphenya ukuvinjelwa kwama-enzyme, ukubopha ama-receptor, kanye nokuguqulwa kwezinqubo ezihlukahlukene zebhayoloji.Ngokuhlola okwengeziwe nokwenza kahle, le nhlanganisela ingase isebenze njengenhlanganisela eholayo yokuthuthukiswa kwezidakamizwa eziqondise umdlavuza, ukuvuvukala, noma ezinye izifo.Izici zayo eziyingqayizivele zesakhiwo kanye nemisebenzi engenzeka yebhayoloji iyenza ibe inhlanganisela ethokozisayo ukuze kwenziwe ucwaningo olwengeziwe kanye nentuthuko emkhakheni wamakhemikhali emithi. I-5-methyl-7-oxo-7,8-dihydropyrido[2,3-d]pyrimidin-2-yl)amino)pyridin-3-yl)piperazine-1-carboxylate inesithembiso njengenhlanganisela eguquguqukayo yokuthuthukiswa kwezidakamizwa.Isakhiwo sayo esiyinkimbinkimbi kanye nemisebenzi engase ibe khona yezokwelapha iyenza ibe ikhandidethi elithakazelisayo ukuze kuqhutshekwe nophenyo njenge-ejenti yokwelapha engase ibe khona ezifweni nezimo ezihlukahlukene.