Oloa

4-[6-(6-bromo-8-cyclopentyl-5-methyl-7-oxo-7,8-dihydro-pyrido[2,3-d]pyrimidin-2-ylamino)-pyridin-3-yl]- piperazine-1-carboxylic acid tert-butyl ester o se faʻapipiʻi e mafai ona faʻaaogaina i suʻesuʻega vailaʻau ma le atinaʻeina o vailaʻau.O lona fausaga lavelave ma vaega galue e ofoina atu avanoa eseese mo suʻesuʻega ma suʻesuʻega o ana faʻaoga togafitiga.O se tasi o faʻaogaina o lenei faʻalapotopotoga o loʻo i totonu o le oncology.O le i ai o le vaega o le bromo ma le pyrido [2,3-d] pyrimidin moiety o loʻo taʻu mai ai e ono i ai le gaioiga o le kanesa.O le vaega o le bromo ua lauiloa ona o lona gafatia e taofia ai le tuputupu aʻe o le sela ma faʻaoso apoptosis i sela o le kanesa.E le gata i lea, o le pyrido [2,3-d] pyrimidin scaffold ua fesoʻotaʻi ma aʻafiaga faʻamaʻi ma faʻamaʻi.O le mea lea, e mafai ona suʻesuʻeina atili lenei faʻalapotopotoga mo lona gafatia e avea o se mea fou e faʻamaʻi ai le kanesa. - fai'ai pupuni.O lenei meatotino e tatalaina ai le avanoa e faʻaaogaina ai i le atinaʻeina o vailaʻau e faʻatatau i faʻamaʻi o le fatugalemu o le tino, e pei o le neurological disorders.E mafai ona faʻaleleia le faʻaogaina e faʻaleleia ai lona filifilia ma le malosi e faasaga i sini faʻapitoa o loʻo aʻafia i nei faʻamaʻi.Prodrugs o mea faʻapipiʻi e le mafai ona faʻaaogaina e mafai ona liua i ni mea gaogao i totonu o le tino.O le vaega tert-butyl ester e mafai ona avea o se vaega puipuia, puipuia le vave fa'agaoioia o le vaila'au a'o le'i o'o atu i le nofoaga o lo'o mana'omia.O le taimi lava e oʻo atu ai i le mea faʻapitoa poʻo sela, o le vaega ester e mafai ona faʻamavaeina faʻamaʻi, tuʻuina atu le mole mole vailaʻau faʻamalosi. E le gata i lea, o le pyridine ma le pyrimidine moieties o loʻo faʻaalia lona gafatia e avea o se pharmacophore mo le fuafuaina o inhibitors filifilia mo enzymes patino poʻo ni tali.O nei mea e mafai ona maua mai i kinase i G protein-coupled receptors, e faʻatatau i suiga na faia i le fausaga autu.O lenei tuufaatasiga e mafai ona avea o se amataga mo suʻesuʻega o fesoʻotaʻiga-gaoioiga ma taʻitaʻia le faʻaleleia atili e atiaʻe ai le iniseti malosi ma le filifilia mo sini faʻapitoa faʻapitoa. I le aotelega, 4- [6- (6-bromo-8-cyclopentyl-5-methyl-7). -oxo-7,8-dihydro-pyrido [2,3-d] pyrimidin-2-ylamino) -pyridin-3-yl] -piperazine-1-carboxylic acid tert-butyl ester faʻaalia le gafatia i vaega eseese o suʻesuʻega vailaʻau.O lona fausaga tulaga ese ma vaega galue e mafai ona suʻesuʻeina atili mo gaioiga faʻamaʻi-kanesa, fatugalemu o le faʻaogaina o fualaau oona, faʻataʻitaʻiga faʻataʻitaʻiga, ma le filifilia ole enzyme poʻo le faʻasaina o le tali.Fa'aauau su'esu'ega ma fa'ata'ita'iga lelei o lenei fa'aputuga e ono ta'ita'i atu ai i le su'esu'eina o ni togafiti fa'afoma'i fou fa'atasi ai ma le fa'aleleia atili o le aoga ma le fa'atatau tonu.