Alaabta

6-Acetyl-8-cyclopentyl-5-methyl-2-[5- (1-piperazinyl) -2-pyridinyl] amino] pyrido [2,3-d] pyrimidin-7 (8H) -hal hydrochloride waa iskudhis oo leh codsiyada suurtagalka ah ee cilmi-baarista dawooyinka iyo horumarinta daroogada.Qaab dhismeedkeeda molecular ee gaarka ah ayaa bixiya fursado lagu baaro adeegsigeeda daawayntaJoogitaanka kooxda acetyl waxay soo jeedinaysaa isdhexgalka suurtagalka ah ee enzymes ee ku lug leh hababka gacanta.Waxaa laga yaabaa inay saameyn ku yeelato enzymes sida kinases ama proteases, taasoo ka dhigaysa musharax rajo leh oo loogu talagalay horumarinta enzymes-gaar ah inhibitors. Kooxaha cyclopentyl iyo methyl ee qaab-dhismeedka ayaa gacan ka geysta dabeecadda lipophilic ee xarunta.Hantidani waxay u oggolaanaysaa inay si fudud u gudubto caqabadaha noolaha, iyada oo kordhinaysa kartideeda musharraxnimada daroogada.Waxaa laga yaabaa in ay xoojisay qulqulka iyo bioavailability, taas oo ka dhigaysa mid ku habboon maamulka afka iyo qaybinta nidaamka.Kooxaha 1-piperazinyl iyo 2-pyridinyl ee ku jira xaruntu waxay bixiyaan faa'iido u leh isticmaalka suurtagalka ah ee naqshadeynta daroogada.Qaybaha Piperazine ayaa si weyn loogu aqoonsaday kimisteriga daawaynta hawlahooda bayooloji.Kooxda piperazine waxay gacan ka geysan kartaa isku-xirnaanta soo-dhoweynta waxayna wax ka beddeleysaa guryaha farmashiyaha.Waxaa intaa dheer, kooxda pyridine waxay inta badan ku lug leedahay isdhexgalka ligand-receptor, maadaama nidaamyada giraanta pyridine ay samayn karaan curaarta hydrogen oo leh goobo gaar ah.Guryahaani waxay ka dhigayaan xaruntan isku xirnaanta suurtagalka ah ee soo-dhoweeyayaasha kala duwan, oo ay ku jiraan G-proteins-ku-ku-duuban reseptors.Tixgelinta pyrido [2,3-d] pyrimidinone scaffold iyo joogitaanka kooxda piperazine, xarunta waxaa loo sahamin karaa sida wakiilka kansarka ka hortagga. .Waxa laga yaabaa inay soo bandhigto saamaynta cytotoxic ee ka dhanka ah unugyada kansarka iyada oo la joojinayo waddooyinka calaamadaynta gaarka ah ee la xidhiidha kororka unugyada.Daraasado dheeraad ah oo ku lug leh moodooyinka vitro iyo in vivo waxay qiimeyn karaan kartidooda sida wakiilka ka hortagga burooyinka. Intaa waxaa dheer, pyrido [2,3-d] pyrimidinone xudunta ayaa la bedeli karaa si loo beegsado cuduro gaar ah ama xaalado.Marka la soo bandhigo kooxaha ku habboon ama beddelka, doorashadooda iyo awooddooda waa la wanaajin karaa, taas oo u oggolaanaysa horumarinta wakiilada daaweynta aadka u gaarka ah. piperazinyl)-2-pyridinyl]amino] pyrido [2,3-d] pyrimidin-7(8H) -hal hydrochloride ayaa awood u leh meelo badan oo cilmi baaris dawo ah.Sifooyinkeeda qaabdhismeedku waxay u oggolaanayaan in la baaro xannibaadda ensaymka, xidhitaanka reseptor-ka, iyo dhaqdhaqaaqa ka hortagga kansarka.Sahaminta dheeraadka ah iyo hagaajinta qaabdhismeedkeeda xudunta u ah waxa laga yaabaa inay soo saarto musharixiinta mukhaadaraadka cusub oo leh hufnaan la wanaajiyey iyo gaar ahaan bartilmaameedyada kala duwan ee daaweynta.