P-38 Developing Hybrid Drugs Capable of Activation by Enzymatic Catalysis
Presenter Status
Associate Professor of Chemistry, Chemistry & Biochemistry
Second Presenter Status
Student, Primary Education
Preferred Session
Poster Session
Start Date
26-10-2018 2:00 PM
End Date
26-10-2018 3:00 PM
Presentation Abstract
We are currently working on synthetic methodology focused on making hybrid drugs that can be activated and released in vivo by enzymes. Our approach is based on creating and utilizing mixed acylals – geminal diesters, which can be cleaved by esterases. The mixed acylals are constructed via a one-flask, two-step sequential process involving electrophilic carbonyl addition followed by nucleophilic substitution. We anticipate that once optimized this process can ‘pair up’ a broad diversity of carboxylic acid containing drugs to form single ‘hybrid’ molecular entities.
P-38 Developing Hybrid Drugs Capable of Activation by Enzymatic Catalysis
We are currently working on synthetic methodology focused on making hybrid drugs that can be activated and released in vivo by enzymes. Our approach is based on creating and utilizing mixed acylals – geminal diesters, which can be cleaved by esterases. The mixed acylals are constructed via a one-flask, two-step sequential process involving electrophilic carbonyl addition followed by nucleophilic substitution. We anticipate that once optimized this process can ‘pair up’ a broad diversity of carboxylic acid containing drugs to form single ‘hybrid’ molecular entities.
Acknowledgments
Andrews University Office of Scholarly Research