Zogulitsa

6-Acetyl-8-cyclopentyl-5-methyl-2-[[5-(1-piperazinyl)-2-pyridinyl]amino]pyrido[2,3-d]pyrimidin-7(8H)-one hydrochloride ndi pawiri ndi zomwe zingagwiritsidwe ntchito mu kafukufuku wamankhwala ndi chitukuko cha mankhwala.Mapangidwe ake apadera a mamolekyu amapereka mwayi wofufuza ntchito zake zochizira.Chigawo ichi ndi cha banja la pyrido [2,3-d]pyrimidinone, lomwe laphunziridwa kwambiri chifukwa cha ntchito zake zamankhwala.Kukhalapo kwa gulu la acetyl kukuwonetsa kuyanjana komwe kungachitike ndi ma enzyme omwe amakhudzidwa ndi ma cell.Zitha kukhala ndi zotsatira zolepheretsa ma enzymes monga kinases kapena ma proteases, zomwe zimapangitsa kuti zikhale zodalirika pakupanga ma enzyme-specific inhibitors.Magulu a cyclopentyl ndi methyl mu dongosololi amathandizira kuti pawiri pakhale lipophilic chikhalidwe.Katunduyu amalola kuti adutse mosavuta zotchinga zamoyo, ndikuwonjezera kuthekera kwake ngati wokonda mankhwala.Zitha kukhala zowonjezereka zowonjezereka komanso zowonjezereka, zomwe zimapangitsa kuti zikhale zoyenera kulamulira pakamwa ndi kugawa mwadongosolo.Magulu a 1-piperazinyl ndi 2-pyridinyl omwe amapezeka mumagulu amapereka kusinthasintha kuti athe kugwiritsidwa ntchito popanga mankhwala.Zochokera ku Piperazine zimadziwika kwambiri mu chemistry yamankhwala chifukwa cha zochita zawo zamoyo.Gulu la piperazine likhoza kuthandizira kuti receptor imangirire ndikuwongolera katundu wa pharmacokinetic.Komanso, gulu la pyridine nthawi zambiri limakhudzidwa ndi mgwirizano wa ligand-receptor, monga machitidwe a mphete a pyridine amatha kupanga ma hydrogen bond ndi malo enieni olandirira.Zinthuzi zimapangitsa kuti gululi likhale ligand lomwe lingathe kukhala ndi zovomerezeka zosiyanasiyana, kuphatikizapo mapuloteni a G. Poganizira za pyrido [2,3-d] pyrimidinone scaffold ndi kukhalapo kwa gulu la piperazine, gululi likhoza kufufuzidwa ngati wothandizira khansa. .Itha kuwonetsa zotsatira za cytotoxic motsutsana ndi ma cell a khansa poletsa njira zowonetsera zomwe zimagwirizanitsidwa ndi kuchuluka kwa ma cell.Maphunziro ena okhudzana ndi mu vitro ndi mu vivo akhoza kuyesa mphamvu zake ngati anti-tumor agent.Kuonjezera apo, pyrido yamagulu [2,3-d] pyrimidinone core ikhoza kusinthidwa kuti igwirizane ndi matenda kapena zochitika zinazake.Poyambitsa magulu oyenerera ogwira ntchito kapena olowa m'malo, kusankha kwake ndi potency kumatha kukulitsidwa, kulola kuti pakhale chitukuko cha mankhwala apadera kwambiri. piperazinyl) -2-pyridinyl]amino]pyrido[2,3-d]pyrimidin-7(8H) -one hydrochloride imakhala ndi kuthekera m'madera angapo a kafukufuku wamankhwala.Mapangidwe ake amalola kuti afufuze za kuletsa kwa ma enzyme, kumanga ma receptor, ndi anti-cancer.Kuunikanso ndi kukhathamiritsa kwa kapangidwe kake koyambira kungapereke mwayi kwa anthu omwe akufuna kugwiritsa ntchito mankhwala osokoneza bongo kuti akhale ochita bwino komanso okhazikika pazolinga zosiyanasiyana zachipatala.