FROM SYNTHESIS TO APPLICATION: THE JOURNEY OF BENZODIOXOL DERIVATIVES IN THERAPEUTIC DISCOVERY
Publication Type
Conference Paper
Authors

 

This study focused on synthesizing a novel series of Benzodioxol derivatives, comprising approximately 55 new compounds, with the objective of assessing their biological activities across multiple targets. Through a comprehensive evaluation involving both in vitro and in vivo assays, the analogues were examined for their impact on AMPA receptors, COX enzymes, α-amylase enzymes, and various cancer cell lines. Among these derivatives, select structures demonstrated potent activity on AMPA receptors, indicating their potential as candidates for Parkinsons disease treatment. The series featuring aryl acetate derivatives exhibited significant potency against COX2 enzymes. Furthermore, specific compounds from the acetic acid group and carboxamide derivatives displayed notable activity against α-amylase enzymes in vitro, with promising in vivo results in reducing sugar levels, surpassing the efficacy of the Acarbose positive control. Molecular docking studies were employed to elucidate interactions between benzodiazepine compounds and AMPA receptors, as well as between the aryl acetic acid group and α-amylase enzymes. Theoretical assessments of bioavailability, conducted through Molinspiration calculation and Lipinskis rule of five, aligned well with experimental findings. Overall, this project has uncovered potential drug candidates targeting AMPA receptors for neurological diseases, highlighted Benzodioxole compounds as novel non-steroidal anti-inflammatory agents against COX enzymes, and identified compounds with promising implications for diabetes treatment.

Conference
Conference Title
4th International Conference on General Health Sciences (ICGeHeS)
Conference Country
Turkey
Conference Date
May 2, 2024 - May 5, 2024
Conference Sponsor
ICGeHeS