1. Preliminary studies of 1,5-benzoxazepine derivatives as potential histamine H 3 receptor antagonists.
- Author
-
Stefaniak-Napieralska M, Walczyński K, Iwan M, Korga-Plewko A, Szałaj N, Więckowska A, and Staszewski M
- Subjects
- Butyrylcholinesterase metabolism, Acetylcholinesterase metabolism, Drug Inverse Agonism, Structure-Activity Relationship, Histamine, Receptors, Histamine H3 chemistry
- Abstract
Aims: Our research aimed to evaluate how the rigidification of the characteristic 3-aminopropyloxy linker by incorporating it into 1,5-benzoxazepines affects the potency of histamine H
3 receptor (H3 R) antagonists/inverse agonists. This research constitutes a starting point for the full characterization of the pharmacological properties of this group of compounds. Materials & methods: Several 1,5-benzoxazepine derivatives were synthesized and pharmacologically tested as potential H3 R antagonist/inverse agonists. In a addition, the effect of the derivatives on acetylcholinesterase and butyrylcholinesterase inhibition and cytotoxicity were tested. Results: The studies indicated 1,5-benzoxazepine containing three carbon side chains as a compound for further modification. Conclusion: Further optimization of the lead structure is necessary, which will favorably affect biological targets.- Published
- 2024
- Full Text
- View/download PDF