Lihlahisoa

6-Acetyl-8-cyclopentyl-5-methyl-2-[[5-(1-piperazinyl)-2-pyridinyl]amino]pyrido[2,3-d]pyrimidin-7(8H) -one hydrochloride ke motsoako. ka likopo tse ka bang teng lipatlisisong tsa meriana le nts'etsopele ea lithethefatsi.Sebopeho sa eona se ikhethang sa limolek'hule se fana ka menyetla ea lipatlisiso mabapi le tšebeliso ea eona ea phekolo.Motsoako ona ke oa lelapa la pyrido[2,3-d]pyrimidinone, le ithutoang haholo bakeng sa mesebetsi ea lona ea meriana.Ho ba teng ha sehlopha sa acetyl ho fana ka maikutlo a ho sebelisana ho ka bang teng le li-enzyme tse amehang lits'ebetsong tsa cellular.E ka 'na ea e-ba le liphello tse thibelang li-enzyme tse kang kinases kapa li-protease, e leng se etsang hore e be mokhethoa ea tšepisang bakeng sa nts'etsopele ea li-enzyme-specific inhibitors.Lihlopha tsa cyclopenyl le methyl mohahong li kenya letsoho ho tlhaho ea lipophilic ea motsoako.Thepa ena e e lumella ho tšela mekoallo ea likokoana-hloko habonolo, ho eketsa bokhoni ba eona ba ho ba moemeli oa lithethefatsi.E ka 'na eaba e ntlafalitse ho phunyeletsa le ho ba le bioavailability, e leng se etsang hore e tšoanelehe bakeng sa tsamaiso ea molomo le kabo ea tsamaiso.Lihlopha tsa 1-piperazinyl le 2-pyridinyl tse teng ka har'a motsoako li fana ka mekhoa e mengata bakeng sa tšebeliso ea eona e ka sebelisoang ha ho etsoa lithethefatsi.Li-derivatives tsa Piperazine li tsejoa haholo k'hemistri ea meriana bakeng sa mesebetsi ea tsona ea likokoana-hloko.Sehlopha sa piperazine se ka kenya letsoho ho li-receptor tse tlamang le ho fetola thepa ea pharmacokinetic.Ho feta moo, sehlopha sa pyridine se atisa ho ameha litšebelisanong tsa ligand-receptor, kaha mekhoa ea mehele ea pyridine e ka etsa likamano tsa hydrogen le libaka tse khethehileng tsa ho amohela.Lintho tsena li etsa hore motsoako ona e be li-ligand tse ka 'nang tsa e-ba teng bakeng sa li-receptor tse fapa-fapaneng, ho akarelletsa le li-receptors tsa G protheine. .E ka bonts'a litlamorao tsa cytotoxic khahlano le lisele tsa mofetše ka ho thibela litsela tse ikhethileng tse amanang le ho ata ha lisele.Liphuputso tse ling tse amanang le in vitro le in vivo li ka hlahloba bokhoni ba eona e le moemeli oa anti-tumor.Ho phaella moo, motsoako oa motsoako oa pyrido [2,3-d] pyrimidinone o ka fetoloa ho lebisa tlhokomelo ea mafu kapa maemo a itseng.Ka ho hlahisa lihlopha tse sebetsang hantle kapa li-substituents, khetho ea eona le matla a eona a ka matlafatsoa, ​​e leng ho lumellang nts'etsopele ea li-agent tse khethehileng haholo tsa phekolo. piperazinyl) -2-pyridinyl]amino]pyrido[2,3-d]pyrimidin-7(8H) -one hydrochloride e na le bokhoni libakeng tse ngata tsa lipatlisiso tsa meriana.Likarolo tsa eona tsa sebopeho li lumella lipatlisiso mabapi le thibelo ea enzyme, ho tlama li-receptor, le ts'ebetso e khahlanong le mofets'e.Patlisiso e tsoelang pele le ntlafatso ea sebopeho sa eona sa mantlha e ka fana ka litlhare tse ncha tse nang le ts'ebetso e ntlafalitsoeng le tse ikhethang bakeng sa lipheo tse fapaneng tsa kalafo.