2-((2-Amino-6-oxo-3,6-dihydro-9H-purin-9-yl)methoxy)-3-hydroxypropyl ((benzyloxy)carbonyl)-L-valinate

Cov tshuaj no feem ntau yog cais raws li cov dawb rau tawm -dawb amorphous lossis crystalline hmoov. Nws cov mis molecular yog C22H28N6O7, sib xws rau qhov hnyav molecular ntawm 488.49. Lub melting point tsis yog sharply txhais, nrog decomposition feem ntau tshwm sim saum 180 degree. Qhov ntsuas qhov ceev yog kwv yees li 1.45 g / cm³ nyob rau hauv ambient tej yam kev mob. Nws pom zoo solubility nyob rau hauv polar aprotic kuab tshuaj xws li dimethyl sulfoxide thiab dimethylformamide, nruab nrab solubility nyob rau hauv methanol thiab ethanol, thiab txwv solubility nyob rau hauv dej thiab chlorinated solvents. Cov molecule muaj ntau yam hydrogen daim ntawv cog lus pub dawb thiab txais los ntawm purine puag, carbamate, thiab hydroxyl pawg. Cov pab pawg tiv thaiv benzyloxycarbonyl (Cbz) ruaj khov nyob rau hauv cov xwm txheej yooj yim tab sis nkag tau yooj yim los ntawm hydrogenolysis lossis muaj zog acids. Cia nyob rau hauv cov thawv kaw nruj nreem nyob rau hauv inert cua ntawm qhov kub thiab txias (2-8 degree) yog pom zoo kom tiv thaiv hydrolysis thiab decomposition. Kev sib cuag nrog cov neeg muaj zog oxidizing, muaj zog acids, thiab cov hauv paus yuav tsum zam.

Cov molecule complex no ua ke nrog kev hloov kho guanine nucleobase nrog valine - muab cov amino acid ester los ntawm kev hloov pauv glycerollipid - zoo li txuas. Lub 9- txoj hauj lwm ntawm 2-amino-6-oxopurine (guanine) core bears hloov glycerol moiety, nrog ib hydroxyl koom nrog ether txuas rau purine thiab lwm yam esterified nrog Cbz-tiv thaiv L-valine resue. Cov qauv no ua raws li qhov tshwm sim ntawm nucleoside-lipid conjugates thiab prodrugs tsim los txhim kho cellular xa ntawm nucleoside analogs. Cov guanine feem muab lub peev xwm rau kev sib koom ua ke hauv paus thiab kev lees paub los ntawm cov enzymes koom nrog hauv nucleic acid metabolism. Lub valine ester qhia ob qho tib si amino acid cim thiab benzyl carbamate tiv thaiv pab pawg, uas tuaj yeem raug tshem tawm kom pom cov amine dawb rau kev ua haujlwm ntxiv lossis hloov kho cov tshuaj pharmacokinetic. Qhov no multifunctional qauv sawv cev rau ib tug sophisticated lub tsev thaiv rau tsim antiviral thiab anticancer nucleoside prodrugs.

Nucleoside Prodrug Development

Qhov kev sib xyaw no ua haujlwm zoo li nruab nrab nruab nrab hauv kev sib txuas ntawm lipid- hloov kho nucleoside prodrugs tsim los hla cov txheej txheem tiv thaiv thiab txhim kho qhov ncauj bioavailability. Cov glycerollipid moiety txhim kho daim nyias nyias permeability, thaum lub valine ester tuaj yeem raug tshem tawm los ntawm esterases hauv vivo kom tso tawm cov active nucleoside analog. Cov tswv yim zoo li no tau ua haujlwm los kov yeej cov cellular tsis zoo ntawm cov tshuaj hydrophilic nucleoside.

Antiviral Research Applications

Hloov kho guanosine derivatives suav nrog cov scaffold no tau tshawb xyuas rau kev ua haujlwm tiv thaiv DNA thiab RNA kab mob, suav nrog kab mob siab B thiab herpesviruses. Cov amino acid ester tuaj yeem pab txhawb kev thauj mus los ntawm peptide transporters, thaum lub hauv paus purine ua raws li cov saw terminator tom qab intracellular phosphorylation. Cov qauv sib txawv nyob ib ncig ntawm cov linker thiab kev tiv thaiv cov pab pawg pab kom optimization ntawm antiviral potency thiab selectivity.

Enzyme-Targeted Drug Delivery

Lub valine moiety tau lees paub los ntawm cov amino acid transporters thiab esterases, ua kom lub hom phiaj xa mus rau cov hlwb qhia cov enzymes. Tom qab enzymatic cleavage, tso tawm nucleoside analog tuaj yeem qhib los ntawm kab mob lossis cellular kinases. Txoj hauv kev no yog tshawb nrhiav txhawm rau txhim kho qhov ntsuas ntsuas ntawm nucleoside analogs hauv kev mob qog noj ntshav thiab kis kab mob los ntawm kev tsom mus rau cov tshuaj nquag hauv cov ntaub so ntswg.

Chemical Biology soj ntsuam

Cov pab pawg benzyloxycarbonyl tuaj yeem hloov nrog cov cim npe fluorescent lossis affinity tuav los tsim kev sojntsuam rau kev kawm nucleoside thauj, metabolism, thiab koom ua ke rau hauv nucleic acids. Lub glycerol linker muab cov ntsiab lus txuas ntxiv rau ntau pawg neeg sau xov xwm yam tsis muaj kev cuam tshuam kev lees paub los ntawm lub hom phiaj enzymes. Cov kev sojntsuam zoo li no yog cov cuab yeej tseem ceeb rau elucidating mechanisms ntawm nucleoside tshuaj ua haujlwm thiab tsis kam.

Cim npe nrov: 2-((2-amino-6-oxo-3,6-dihydro-9h-purin-9-yl)methoxy)-3-hydroxypropyl ((benzyloxy)carbonyl)-l-valinate, Suav teb 2-((2-amino-6-oxo-3,6-dihydro-9h-purin-9-yl)methoxy)-3-hydroxypropyl ((benzyloxy)carbonyl)-l-valinate manufacturers, lwm tus neeg