| Autor: |
Moaz M. Abdou, Dewen Dong, Paul M. O'Neill, Eric Amigues, Magdalini Matziari |
| Jazyk: |
angličtina |
| Rok vydání: |
2023 |
| Předmět: |
|
| Zdroj: |
Arabian Journal of Chemistry, Vol 16, Iss 2, Pp 104499- (2023) |
| Druh dokumentu: |
article |
| ISSN: |
1878-5352 |
| DOI: |
10.1016/j.arabjc.2022.104499 |
| Popis: |
In medicinal chemistry for the purpose of lead optimization, hit selection of new isofunctional chemotypes are crucial for the success of identifying novel chemical entities of increased potency. Using fragment-based design approach with the N-selective inhibitor RXP407, a novel phosphinic peptide scaffold that consisted of modified RXP407 fragments was generated. The presented synthetic route is straightforward and produces the desired product Z-RXP407 in moderate yield. The (S,R,S,S)-Z-RXP407 analog has been evaluated for the C- and N-domain constructs of angiotensin-converting enzyme. The potency of this analog has been much lower compared to the parent compound RXP407, providing thus valuable insights regarding further design based on structure–activity relationships. |
| Databáze: |
Directory of Open Access Journals |
| Externí odkaz: |
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