1. Taw qhia
Umifenovir Hydrochloride yog ib qho tshuaj tiv thaiv kab mob khaub thuas ob zaug, uas tuaj yeem tiv thaiv kab mob khaub thuas los ntawm kab mob khaub thuas A thiab B tib lub sijhawm, thiab kuj tseem tuaj yeem muaj kev tiv thaiv kab mob tiv thaiv kab mob ua pa.
Abidor hauv vitro tshuaj tiv thaiv kab mob tau pom tias inhibition ntawm ntau yam kab mob ua pa hauv qab no.
H1N1 thiab H3N2 kab mob khaub thuas tib neeg thiab H9N2 kab mob khaub thuas avian.
Parainfluenza virus type 3 (PIV3).
Herpes simplex virus type 1 (HSV-1).
Enterovirus type EV71 (EV71).
Respiratory syncytial virus (RSV).
Tus kab mob Coxsackie A16 (CoxA16).
2. Lub luag haujlwm tseem ceeb
2. Lub luag haujlwm tseem ceeb
2.1 Anti-influenza virus.
2.1.1 Kev tswj qhov ncauj ntawm Abidor API 90mg / kg / hnub ua rau txo qis lub ntsws Performance index ntawm nas (p<0.01); oral administration of Abidor capsules 45mg/kg/day and tablets 25mg/kg/day significantly reduced the lung index of mice (p<0.05), increased the survival rate of mice (p<0.05) and prolonged the survival time of dead mice (p<0.05). No significant inhibition of viral replication in mouse lung tissue by any of the above three doses of Abidor.
2.2 Anti-inflammatory kev ua.
2.2.1 Abidor API 90 mg/kg/hnub nyob rau hnub 5 tom qab kis kab mob tau pom tias muaj kev cuam tshuam tseem ceeb ntawm kev nce mRNA kev qhia ntawm tus kab mob kis kab mob-induced inflammatory yam CCL2 (p < 0.01) thiab TNF- (p <0.05) nyob rau hauv lub ntsws ntawm nas.
2.2.2 qhia txog kev tswj hwm ntawm mRNA kev qhia ntawm IL-6 (p < 0.05) thiab CXCL9 (p < 0.001).
2.2.3 qee qhov kev txhim kho hauv cov tsos mob ua npaws, txo cov tsos mob ntawm qhov ntswg nrog rau kev ua kom muaj zog hauv ferrets hauv 70 mg / kg / hnub koob tshuaj ntawm Abidor ntsiav tshuaj
2.2.4 Hnub 3 tom qab kis kab mob, kev kho Abidor tsis cuam tshuam cov kab mob sib kis hauv ferret nasal turbinate, trachea, ntsws cov ntaub so ntswg thiab qhov ntswg lavage kua, tab sis tseem inhibited TNF, IL-10 (p<0.001), CXCL8 (p<0.001), IL-6 (p<0.01), IL-4 (p<0.001), IL-1β (p<0.01) , TGF-β (p < 0.01) and IFN-α (p < 0.01) and other cytokine mRNA expressions were elevated.
2.2.5 Tom qab hnub 6 ntawm kev kis tus kab mob, kev kho Abidor tau pom qee qhov kev txhim kho hauv cov cell infiltration thiab ntsws interstitial widening hauv ferret ntsws cov ntaub so ntswg.
Cov ntsiab lus: Abirater muaj qhov dav-spectrum inhibitory cuam tshuam rau cov kab mob ua pa, uas pib elucidates lub immunomodulatory-raws li kev ua ntawm Abirater hauv vivo, thiab nws inhibition ntawm tus kab mob khaub thuas HA2-kuaj membrane fusion.
Mechanism
Abidor muaj qhov sib txawv ntawm kev ua haujlwm rau lwm cov tshuaj tiv thaiv ib leeg.
Tib lub hom phiaj tshuaj tiv thaiv kab mob xws li neuraminidase inhibitors (oseltamivir) thiab HIV protease inhibitors (ritonavir) muaj tib lub tswv yim ntawm kev ua thiab tej zaum yuav muaj kev cuam tshuam los ntawm kev siv tshuaj kho mob, thaum cov kab mob ua rau muaj kev hloov pauv thiab kev kho mob yuav nyuaj heev thaum muaj kev tiv thaiv kab mob. dhau los ua neeg nyob.
Abidor tau siv los kho tus mob khaub thuas rau ntau tshaj 10 xyoo thiab tsis muaj kev tiv thaiv tau raug tshaj tawm lossis pom hauv cov pejxeem. Qhov no qhia tau hais tias, tsis zoo li ib lub hom phiaj antivirals, Abidor muaj ntau yam tshuaj tiv thaiv kab mob. Qhov kev txiav txim ncaj qha ntawm tus kab mob tuaj yeem cuam tshuam tsis tau tsuas yog nrog cov adsorption ntawm tus kab mob, tab sis kuj nrog tus kab mob decapitation thiab kev cuam tshuam ntawm cov kab mob protein nrog cov kab mob organelle.
Paub cov txheej txheem ntawm kev ua haujlwm uas feem ntau tiv thaiv kab mob khaub thuas
1) Thaiv tus kab mob nkag: Endocytosis: Abidor inhibits tus kab mob nkag los ntawm kev cuam tshuam nrog lattice-protein-dependent endocytosis. Thaiv fusion: Abidor inhibits fusion ntawm cov kab mob lipid daim nyias nyias nrog endocytic vesicle membranes, ua raws li daim nyias nyias fusion inhibitor. Ua tsaug rau qhov kev ua haujlwm no, Abidor muaj cov tshuaj tiv thaiv kab mob dav dua li oseltamivir.
(ii) Interferon induction: Abirater induces interferon ntau lawm los ntawm activating 2, 5-oligoadenylate synthase (OAS), uas degrades viral mRNA thiab tiv thaiv kab mob replication. Nws muaj cov nyhuv interferon-inducing muaj zog, inducing ib tug txaus npaum li cas ntawm interferon yuav tsum tau tsim nyob rau hauv lub zos mucosa ntawm lub pa ib ntsuj av tau nyob rau hauv ib tug luv luv lub sij hawm ntawm lub sij hawm (24 h) thiab tsim ib tug broad-spectrum antiviral xeev nyob rau hauv lub ua pa ib hnub. 4. Nws txhim kho lub cev tiv thaiv kab mob thiab muaj peev xwm engulf tus kab mob, sai dua lub sij hawm nws yuav siv sij hawm rau cov tshuaj tiv thaiv (feem ntau yog 14 d).
(iii) Boosts lub cev tiv thaiv kab mob: Abidor activates phagocytes thiab txhim khu kev tiv thaiv tsis tshwj xeeb. Abidor muaj kev txhim kho tseem ceeb hauv ntau qhov kev tiv thaiv kab mob (CD4 ntxiv, CD8 ntxiv, B hlwb thiab cov tshuaj tiv thaiv kab mob ntshav qab zib) hauv cov neeg mob immunocompromised.
Lwm yam tsis paub txog kev ua haujlwm los thaiv cov kab mob nkag mus rau hauv cov hlwb
Raws li Abidor yog cov tshuaj tiv thaiv kab mob dav dav, nrog rau kev tiv thaiv kab mob tsis yog tsuas yog tiv thaiv kab mob khaub thuas xwb tab sis kuj muaj lwm yam kab mob ua pa (tus kab mob ua pa syncytial, tus kab mob parainfluenza, rhinovirus, coronavirus, thiab lwm yam), nws muaj ntau yam kev ua haujlwm hauv kev tiv thaiv kab mob los ntawm nkag mus rau hauv hlwb (nyob rau hauv cov ntaub ntawv ntawm tus kab mob khaub thuas, nws cuam tshuam rau kev nkag mus ntawm cov kab mob los ntawm HE (Hemagglutinin acetylesterase) receptor), thiab ntxiv cov txheej txheem los tiv thaiv kev nkag mus ntawm cov kab mob sib txawv yuav raug tshawb xyuas ntxiv.
Piv nrog rau lwm cov tshuaj tiv thaiv kab mob, Umifenovir Hydrochloride muaj cov yam ntxwv hauv qab no:
1. Tua kab mob khaub thuas A thiab B tib lub sijhawm.
2. Tiv thaiv kab mob fusion thiab replication.
3. Induces interferon thiab pom tseeb txhim kho tus kheej tiv thaiv.
4. txo cov tsos mob ntawm tus mob khaub thuas thiab txo cov kab mob khaub thuas.
5. Tiv thaiv qhov tshwm sim thiab kev loj hlob ntawm tus mob khaub thuas lig.
6. Noj thaum muaj kab mob khaub thuas kis tau zoo tuaj yeem tiv thaiv tus mob khaub thuas.
7. Hauv vitro kuaj, nws muaj kev kho mob ntawm tus kab mob SARS thiab tus kab mob khaub thuas avian.
8. Kev tswj xyuas qhov ncauj yooj yim, kev nyab xeeb siab thiab ua raws li qhov zoo.
3. Cov ntawv thov
Umifenovir Hydrochloride yog siv rau hauv cov tshuaj rau cov neeg laus thiab cov menyuam yaus uas muaj mob khaub thuas A, mob khaub thuas B, mob khaub thuas ua pa kab mob, mob ua pa nyuaj, nrog rau kev tiv thaiv thiab kev kho mob ntawm cov mob bronchitis thiab mob ntsws.
4. Flow Chart
Siv 3-iodo-4-nitrophenol ua raw khoom, lub compound yog npaj los ntawm hydroxyl cov tshuaj tiv thaiv nrog acetyl chloride → Cov compound yog hloov nrog ethyl acetoacetate nyob rau hauv qhov kev txiav txim ntawm lub hauv paus los npaj cov compound → Compound yog synthesized los ntawm kev txo qis-condensation synergistic cov tshuaj tiv thaiv nyob rau hauv cov xwm txheej ntawm acetic acid thiab hlau hmoov rau synthesize indole nplhaib kom tau compound → Compound yog npaj los ntawm N-methylation cov tshuaj tiv thaiv nrog dimethyl sulfate → Compound yog tau nyob rau hauv carbon tetrachloride, lub compound yog npaj los ntawm dibromination nrog bromine → Lub compound yog reacted nrog thiophenol nyob rau hauv alkaline tej yam kev mob, thiab cov compound yog tau tom qab acidification; → Lub compound nyob rau hauv cov tshuaj tiv thaiv hnyav muaj dimethylamine Nyob rau hauv lub xub ntiag ntawm ib tug aqueous tov ntawm formaldehyde, lub compound yog npaj → Cov compound yog acidified nyob rau hauv kub acetone kom tau Arbidol hydrochloride
5. Tus Qauv Zoo
Cov khoom | Specifications | Cov txiaj ntsig |
Qhov tshwm sim | Dawb los yog yuav luag dawb hmoov | Yuav luag dawb hmoov |
Absorption yam | Yuav tsum yog 385-409 | 399 |
Kev txheeb xyuas | ||
1 | Yuav tsum tsim txiv kab ntxwv liab precipitate | Ua raws |
2 | Nyob rau hauv chromatogram ntawm kev txiav txim siab cov ntsiab lus, lub sij hawm tuav ntawm lub ntsiab ncov ntawm cov qauv kev daws yuav tsum ua raws li cov qauv kev daws teeb meem. | Ua raws |
3 | Infrared absorption spectra yuav tsum ua raws li cov qauv qauv. | Ua raws |
4 | Kev txheeb xyuas cov tshuaj tiv thaiv ntawm filtrate yuav tsum yog chloride. | Ua raws |
Kev sim | ||
Qhia meej thiab xim ntawm ethanol tov | daws clarity yuav tsum tsawg dua No.1 turbidity standard tov. | Ua raws |
Cov xim yuav tsum sib dua li No.3 daj ntsuab los yog No.3 xim av liab xim qauv xim. | Ua raws | |
Ph | 4.0 - 6.0 | 4.3 |
Hlawv residue | Tsawg dua los yog sib npaug rau 0.2 feem pua | 0.1 feem pua |
Dej | 3.0 feem pua - 4 0 feem pua | 3.4 feem pua |
Cov hlau hnyav | Tsawg dua lossis sib npaug li 10 ppm | <10ppm |
Residual kuab tshuaj | Ethanol Tsawg dua lossis sib npaug rau 0.5 feem pua | 0.02 feem pua |
Acetone Tsawg dua lossis sib npaug rau 0.5 feem pua | 0.01 feem pua | |
Cov khoom muaj feem xyuam | Ib qho impurity Tsawg dua lossis sib npaug rau 0.5 feem pua | 0.2 feem pua |
Tag nrho impurity Tsawg dua lossis sib npaug rau 1.0 feem pua | 0.6 feem pua | |
Kab mob | Tag nrho cov kab mob aerobic Tsawg dua lossis sib npaug li 1000cfu / g | 20 cfu/g |
Tag nrho cov naj npawb ntawm mucedines thiab poov xab Tsawg dua lossis sib npaug li 100 cfu / g | <10cfu/g | |
Assay | Tsis pub tsawg dua 98.0 feem pua thiab tsis pub ntau tshaj 102.0 feem pua ntawm cov dej tsis muaj dej, Muab xam li C22H25BRN2O3S·HCI | 100.3 feem pua |
6. Txoj kev tsom xam
MOA muaj nyob rau thaum thov
7. Siv Chromatogram
Spectrum muaj nyob rau thaum thov
8. Kev ruaj ntseg thiab kev nyab xeeb
Kev ruaj ntseg:
Nyob ruaj khov nyob rau hauv cov xwm txheej zoo (chav kub). Cov Ntaub Ntawv Kev ruaj ntseg muaj nyob rau ntawm koj qhov kev thov.
Kev nyab xeeb:
Raws li GARS (Feem ntau Pom Zoo Raws Li Kev Nyab Xeeb) Daim Ntawv Ceeb Toom ntawm Teb Chaws Asmeskas, nws muaj kev nyab xeeb rau tib neeg noj.
9. Cov neeg siv lus pom
10. Peb Daim Ntawv Pov Thawj
11. Peb Cov Neeg Siv Khoom
12. Exhibition
Cim npe nrov: umifenovir hydrochloride cas 131707-23-8, manufacturers, lwm tus neeg, Hoobkas, lag luam wholesale, yuav, nqe, zoo tshaj plaws, tej, kev muag khoom
