Oloa

6-Acetyl-8-cyclopentyl-5-methyl-2-[[5-(1-piperazinyl)-2-pyridinyl]amino]pyrido[2,3-d]pyrimidin-7(8H)-one hydrochloride o se tuufaatasiga fa'atasi ai ma fa'aoga talafeagai i su'esu'ega fa'afoma'i ma le atina'eina o vaila'au.O lona fausaga mole mole tulaga ese e maua ai avanoa mo suʻesuʻega i ana faʻaoga faʻapitoa.O lenei faʻapipiʻi e aʻafia i le aiga pyrido [2,3-d] pyrimidinone, lea na suʻesuʻeina lautele mo ana gaioiga faʻafomaʻi.O le i ai o le vaega acetyl o loʻo fautua mai ai fegalegaleaiga faʻatasi ma enzymes e aʻafia i gaioiga feaveaʻi.E ono iai ni a'afiaga fa'alavelave i enzymes pei o kinases po'o protease, ma avea ai ma sui tauva mo le atina'eina o inhibitors fa'apitoa ole enzyme.O vaega o le cyclopentyl ma le methyl i totonu o le fausaga e saofagā i le natura lipophilic o le tuufaatasiga.O lenei meatotino e mafai ai ona faigofie ona sopoia pa puipui o meaola, faʻateleina lona gafatia e avea ma sui o vailaʻau.Atonu e faʻaleleia atili le faʻaogaina ma le bioavailability, e talafeagai mo le faʻaogaina o le tautala ma le tufatufaina atu o le tino. O vaega 1-piperazinyl ma 2-pyridinyl o loʻo iai i totonu o le faʻalapotopotoga e maua ai le faʻaogaina mo lona faʻaogaina i le mamanu o fualaau faasaina.Piperazine derivatives e lauiloa lautele i vailaʻau kemisi mo a latou gaioiga olaola.Ole vaega ole piperazine e mafai ona saofagā ile faʻamaufaʻailogaina ma faʻaogaina mea tau vailaʻau.E le gata i lea, o le vaega o le pyridine e masani ona aʻafia i fegalegaleaiga ligand-receptor, e pei o le pyridine ring system e mafai ona fausia ai le hydrogen faʻatasi ma nofoaga faʻapitoa e maua ai.O nei mea totino e avea ai lenei mea faʻapipiʻi o se ligand e mafai ona faʻaogaina mo le tele o tali, e aofia ai le G protein-coupled receptors. Mafaufau i le pyrido [2,3-d] pyrimidinone scaffold ma le i ai o le piperazine group, e mafai ona suʻesuʻeina le faʻapipiʻi e fai ma sui o le kanesa. .E ono fa'aalia ai a'afiaga o le cytotoxic i sela o le kanesa e ala i le taofiofia o ala fa'ailo fa'apitoa e feso'ota'i ma le fa'ateleina o sela.O isi suʻesuʻega e aofia ai in vitro ma in vivo faʻataʻitaʻiga e mafai ona iloilo lona gafatia e avea o se anti-tumor agent. E le gata i lea, o le pyrido [2,3-d] pyrimidinone core e mafai ona faʻaleleia e faʻatatau i faʻamaʻi faʻapitoa poʻo tulaga.E ala i le faʻalauiloaina o vaega faʻatino talafeagai poʻo mea e suitulaga, e mafai ona faʻaleleia lona filifilia ma le malosi, faʻatagaina mo le atinaʻeina o vailaʻau faʻapitoa faʻapitoa. I le aotelega, 6-Acetyl-8-cyclopentyl-5-methyl-2-[[5-(1- piperazinyl) -2-pyridinyl] amino] pyrido [2,3-d] pyrimidin-7 (8H) -one hydrochloride umia le gafatia i le tele o vaega o suʻesuʻega vailaʻau.O ona foliga fa'atulagaina e mafai ai ona su'esu'eina le fa'asaina o le enzyme, fa'amauina o le talitali, ma le gaioiga e fa'ato'ilalo ai le kanesa.O le su'esu'eina atili ma le fa'ata'ita'iina o lona fausaga autu e mafai ona maua mai ai ni tala fou mo fualaau fa'asaina ma le fa'aleleia atili o le aoga ma le fa'apitoa mo togafitiga fa'apitoa.