Project No. | LZP-2021/1-0578 |
|---|---|
Project coordinator
| Latvian Institute of Organic Synthesis (LIOS) |
Project manager | Prof. Edgars Sūna (LIOS) |
Projekta īstenošanas ilgums | 36 months (2022-2024) |
Total cost | 299 999,70 EUR |
Drug development is a painstaking process iteratively progressing through the stages of hit discovery, hit-to-lead and lead optimization followed by identification of a clinical candidate. To mitigate problems arising during the drug development process, bioisoteric replacement is often used. This project is intended to explore synthetic routes towards sulfur-based bioisosteres of γ-lactams, the scaffold ubiquitously present in bioactive molecules.
The project aims to develop methods for stereoselective synthesis of potential drug molecules. These synthetic approaches will be used to develop next generation analogues for neuroprotective drugs.
Project Progress
The following research activities were carried out during the reporting period:
- Synthesis of substrates for the scope evaluation of the developed SN2’-type cyclization methodology for the synthesis of 5-membered cyclic sulfinamides (WP1);
- Characterization of target products and intermediates (WP1);
- Synthetic modifications of the cyclic sulfinamide scaffold (WP1).
Publication date 04.04.2022.
The following research activities were carried out during the reporting period:
- Characterization of target products and intermediates for SN2’-type cyclization methodology for the synthesis of 5-membered cyclic sulfinamides (WP1);
- Writing and submitting a publication manuscript on the SN2’ cyclization methodology for the synthesis of 5-membered cyclic sulfinamides (WP4);
- Optimization studies for the synthesis of 5-membered cyclic sulfinamides using SN2-type cyclization approach (WP2).
Publication date 04.07.2022.
- Optimization studies for the synthesis of 5-membered cyclic sulfinamides using SN2-type cyclization approach (WP2);
- Participation and poster presentation at the Balticum Organicum Syntheticum 2022 conference (Gļebs Jeršovs, WP4).
The following research activities were carried out during the reporting period:
- Optimization studies for the synthesis of 5-membered cyclic sulfinamides using SN2-type cyclization approach (WP2);
- Synthesis of cyclic sulfinamide-derived E1R analogs (WP3).
Publication date 03.01.2023.
- Synthesis of cyclic sulfinamide-derived E1R analogs and their ex-vivo evaluation (WP3);
- The development of methodology for Zn-carbenoid-mediated S-alkylation of sulfinamides: optimization studies on the model substrates.
- Synthesis of cyclic sulfinamide-derived analogs or Rolipram (WP3);
- The development of methodology for Zn-carbenoid-mediated S-alkylation of sulfinamides: investigating the generality of the approach by screening different gem-diiodides and various Ellman’s sulfinamide derivatives under the developed conditions (WP2);
- Participation and poster presentation at 23rd Tetrahedron Symposium (Gļebs Jeršovs, WP4).