Ibicuruzwa

6-Acetyl-8-cyclopentyl-5-methyl-2 - [[5- (1-piperazinyl) -2-pyridinyl] amino] pyrido hamwe nibisabwa mubushakashatsi bwa farumasi no guteza imbere imiti.Imiterere yihariye ya molekile itanga amahirwe yo gukora iperereza kumikoreshereze yubuvuzi.Iyi nteruro ni iyumuryango wa pyrido [2,3-d] umuryango wa pyrimidinone, wakozweho ubushakashatsi kubikorwa bya farumasi.Kubaho kwa acetyl byerekana imikoranire ishobora kuba na enzymes zigira uruhare mubikorwa bya selile.Irashobora kugira ingaruka zibuza imisemburo nka kinase cyangwa protease, bigatuma iba umukandida utanga ikizere cyo guteza imbere inzitizi zihariye za enzyme. Amatsinda ya cyclopentyl na methyl mumiterere agira uruhare muri kamere ya lipofilique.Uyu mutungo uyemerera kunyura mu buryo bworoshye inzitizi zishingiye ku binyabuzima, byongera ubushobozi bwawo nk'umukandida w'ibiyobyabwenge.Irashobora kuba yarongereye ubushobozi bwa bioavailability, bigatuma ikwiranye nubuyobozi bwo munwa no gukwirakwiza sisitemu.Itsinda rya 1-piperazinyl na 2-pyridinyl biboneka muruganda ritanga uburyo bwinshi bwo gukoresha muburyo bwo gukoresha ibiyobyabwenge.Ibikomoka kuri Piperazine bizwi cyane muri chimie yubuvuzi kubikorwa byabo byibinyabuzima.Itsinda rya piperazine rishobora kugira uruhare mu guhuza reseptor no guhindura imiti ya farumasi.Byongeye kandi, itsinda rya pyridine rikunze kugira uruhare mubikorwa bya ligand-reseptor, kuko sisitemu yimpeta ya pyridine irashobora gukora hydrogène ihuza urubuga rwihariye.Iyi mitungo ituma iyi nteruro ishobora kuba ligand kubakira bitandukanye, harimo na proteine ​​zifatanije na G. Urebye pyrido [2,3-d] pyrimidinone scafold no kuba hari itsinda rya piperazine, uruganda rushobora gushakishwa nkumukozi urwanya kanseri. .Irashobora kwerekana ingaruka za cytotoxic zirwanya kanseri binyuze mukubuza inzira zihariye zerekana ibimenyetso bifitanye isano no gukwirakwiza selile.Ubundi bushakashatsi bujyanye na vitro no muri moderi ya vivo burashobora gusuzuma ubushobozi bwayo nkumuti urwanya ibibyimba.Ikindi kandi, pyrido [2,3-d] pyrimidinone yibigize irashobora guhinduka kugirango yibasire indwara cyangwa ibihe byihariye.Mugutangiza amatsinda akwiye cyangwa insimburangingo, guhitamo kwayo nimbaraga birashobora kunozwa, bigatuma habaho iterambere ryimiti yihariye yo kuvura.Mu ncamake, 6-Acetyl-8-cyclopentyl-5-methyl-2 - [[5- (1- piperazinyl) -2-pyridinyl] amino] pyrido [2,3-d] pyrimidin-7 (8H)-hydrochloride imwe ifite ubushobozi mubice byinshi byubushakashatsi bwa farumasi.Imiterere yimiterere yemerera gukora iperereza kubuza enzyme, guhuza reseptor, nibikorwa byo kurwanya kanseri.Ubundi bushakashatsi no kunoza imiterere yabwo birashobora gutanga abakandida bashya b'ibiyobyabwenge bafite imikorere myiza kandi yihariye intego zitandukanye zo kuvura.