Iimveliso

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 yikhompawundi enesakhono esikhulu kumachiza amayeza kunye nophuhliso lwamachiza.Isakhiwo sayo se-molecular esiyinkimbinkimbi sicebisa ngeendlela ezahlukeneyo ezinokuthi zenze izicelo.Le ngqungquthela iqulethe i-piperazine-1-carboxylate core, esetyenziswa ngokuqhelekileyo kwi-scaffold kwi-chemistry yamayeza ngenxa yendalo yayo eguquguqukayo kunye noluhlu olubanzi lwamathuba okujoliswa kweziyobisi.Ubukho be-piperazine moiety buvumela ukusebenzisana kunye nama-receptors ahlukeneyo kunye ne-enzymes, okwenza kube ngumviwa onomdla wokuphuhliswa kwee-agent zonyango.I-6-(1-butoxyvinyl) -8-cyclopentyl-5-methyl-7-oxo-7, I-8-dihydropyrido [2,3-d] pyrimidin-2-yl iqela kwisakhiwo libonelela ngemisebenzi enokubakho ye-pharmacological.Ezo pyrido [2,3-d] pyrimidine derivatives ziye zafundwa ngokubanzi kwiipropati zabo zokuchasa, i-antiviral, kunye ne-anticancer.Amaqela e-cyclopenyl kunye ne-methyl afaka isandla kwi-lipophilicity ye-compound, enokuphucula ukunyanzeliswa kweselula kunye ne-bioavailability.Iqela le-tert-butyl ester libonelela ngokuzinza kwi-compound kwaye linokuguqulwa ngokulula kwamanye amaqela asebenzayo, okuvumela ukuguqulwa okuqhubekayo okanye ukukhutshwa.Oku kuguquguquka kubaluleke kakhulu kwimichiza yonyango, njengoko kwenza ukuba kuphuhliswe iikhompawundi ezinamandla kunye nezikhethiweyo.Iqela le-pyridin-3-yl kwisakhiwo lisebenza njenge-ligand enokubakho kwii-receptors ezahlukeneyo, ezifana ne-G protein-coupled receptors (GPCRs).Oku kuphakamisa ukuba i-compound ingaba nefuthe kwiindlela zokubonisa i-intracellular kwaye ingaphononongwa ngakumbi ngokukwazi kwayo njenge-modulator okanye umchasi we-receptors ethile echaphazelekayo kwiimeko zesifo.Isakhiwo esipheleleyo 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 amanqaku aphezulu amandla ayo ekuphuhlisweni kwezonyango ezinoveli.Inika amathuba okuphanda inhibition ye-enzyme, ukubopha i-receptor, kunye nokumodareyithwa kweenkqubo ezahlukeneyo zebhayoloji.Ngokuphononongwa ngakumbi kunye nokuphucula, le khompawundi inokuthi isebenze njengekhompawundi ekhokelayo ekuphuhlisweni kweziyobisi ezijolise kumhlaza, ukudumba, okanye ezinye izifo.Iimpawu zayo ezikhethekileyo zesakhiwo kunye nemisebenzi yebhayoloji enokubakho iyenza ibe yikhompawundi enomdla kuphando olongezelelweyo kunye nophuhliso kwicandelo lemichiza yamayeza.Ekuqukumbeleni, i-tert-butyl 4-(6-((6-(1-butoxyvinyl)-8-cyclopentyl-) I-5-methyl-7-oxo-7,8-dihydropyrido[2,3-d]pyrimidin-2-yl)amino)pyridin-3-yl)piperazine-1-carboxylate ibambe isithembiso njengekhompawundi eguquguqukayo yokuphuhliswa kweziyobisi.Ubume bayo obuntsonkothileyo kunye nemisebenzi enokubakho ye-pharmacological yenza ukuba ibe ngumviwa onomdla wophando olongezelelweyo njenge-arhente yonyango enokubakho kwizifo ezahlukeneyo kunye neemeko.