ALL libraries (COBIB.SI union bibliographic/catalogue database)
-
Sinteza izoksazolopirimidinskih agonistov Tollu podobnega receptorja 7 z različnimi substitucijami na izoksazolnem obroču = Synthesis of isoxazolopyrimidine Toll-like receptor 7 agonists with different substitutions on the isoxazole ring : Uniform Master's Study Programme PharmacySlokan, TjašaTollu podobni receptorji (TLR) so pomembna skupina receptorjev, ki igrajo ključno vlogo v prirojenem in pridobljenem imunskem sistemu. So obetavne tarče za zdravljenje okužb, avtoimunskih bolezni in ... raka. Pri človeku so do sedaj odkrili 10 različnih tipov TLR. V okviru magistrske naloge smo se osredotočili na TLR7, ki je endosomski receptor in prepoznava enoverižno RNA virusov. S TLR7 povzročena aktivacija imunskega sistema privede do protivnetnega, protivirusnega in protitumornega delovanja, zato TLR7 predstavlja potencialno tarčo za zdravljenje virusnih okužb, alergijske astme in rakavih obolenj. Na podlagi znanega TLR7 agonista 3-(4-fluorofenil)-4-(3-metilpiperidin-1-il)-6- (trifluorometil)izoksazolo[5,4-d]pirimidina smo načrtovali in sintetizirali 11 novih potencialnih agonistov TLR7. Za sintezo analogov 6-(trifluorometil)izoksazolo[5,4-d]pirimidina z različnimi substitucijami na izoksazolnem obroču smo uporabili šeststopenjski sintezni postopek. Končne spojine smo ovrednotili na humani celični liniji HEK293. Določili smo jim topnost v DMSO in celičnem mediju, citotoksičnost ter preverili njihovo agonistično delovanje na TLR7. Ugotovili smo, da so vse sintetizirane spojine zaradi svoje lipofilnosti slabo topne v celičnem mediju. Posledično so bili preliminarni testi agonizma izvedeni pri nizkih koncentracijah, kar je vplivalo na jakost agonističnega delovanja na TLR7. Spojine z izobutilaminskim fragmentom na pirimidinskem obroču (37, 38, 40 in 41), so se izkazale za citotoksične. Izmed vseh sintetiziranih spojin je le 3-(4-klorofenil)-4-(3-metilpiperidin-1-il)-6- (trifluorometil)izoksazolo[5,4-d]pirimidin (35) izkazoval agonistično delovanje na TLR7 z vrednostjo EC50 21,4 μM. Spojina 35 predstavlja dobro izhodišče za nadaljno optimizacijo, predvsem v smislu izboljšanja fizikalno-kemijskih lastnosti.Type of material - master's thesis ; adult, seriousPublication and manufacture - Ljubljana : [T. Slokan], 2022Language - slovenianCOBISS.SI-ID - 124073987
Author
Slokan, Tjaša
Other authors
Sova, Matej, 1979- |
Strašek Benedik, Nika
Topics
Imunski sistem |
Tollu-podobni receptorji |
TLR7 |
agonist |
6-(trifluorometil)izoksazolo[5, 4- d]pirimidin
![loading ... loading ...](themes/default/img/ajax-loading.gif)
Library/institution |
City | Acronym | For loan | Other holdings |
---|---|---|---|---|
Faculty of Pharmacy, Ljubljana | Ljubljana | FFALJ |
reading room 1 cop.
|
![loading ... loading ...](themes/default/img/ajax-loading.gif)
![loading ... loading ...](themes/default/img/ajax-loading.gif)
![loading ... loading ...](themes/default/img/ajax-loading.gif)
Shelf entry
Permalink
- URL:
Impact factor
Access to the JCR database is permitted only to users from Slovenia. Your current IP address is not on the list of IP addresses with access permission, and authentication with the relevant AAI accout is required.
Year | Impact factor | Edition | Category | Classification | ||||
---|---|---|---|---|---|---|---|---|
JCR | SNIP | JCR | SNIP | JCR | SNIP | JCR | SNIP |
Select the library membership card:
If the library membership card is not in the list,
add a new one.
DRS, in which the journal is indexed
Database name | Field | Year |
---|
Links to authors' personal bibliographies | Links to information on researchers in the SICRIS system |
---|---|
Slokan, Tjaša | ![]() |
Sova, Matej, 1979- | 25490 |
Strašek Benedik, Nika | 52378 |
Source: Personal bibliographies
and: SICRIS
Select pickup location:
Material pickup by post
Delivery address:
Address is missing from the member's data.
The address retrieval service is currently unavailable, please try again.
By clicking the "OK" button, you will confirm the pickup location selected above and complete the reservation process.
By clicking the "OK" button, you will confirm the above pickup location and delivery address, and complete the reservation process.
By clicking the "OK" button, you will confirm the address selected above and complete the reservation process.
Notification
Automatic login and reservation service currently not available. You can reserve the material on the Biblos portal or try again here later.
Subject headings in COBISS General List of Subject Headings
Select pickup location
The material from the parent unit is free. If the material is delivered to the pickup location from another unit, the library may charge you for this service.
Pickup location | Material status | Reservation |
---|
Reservation in progress
Please wait a moment.
Reservation was successful.
Reservation failed.
Reservation...
Membership card:
Pickup location: