Presentation Title

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.

Acknowledgments

Andrews University Office of Scholarly Research

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Oct 26th, 2:00 PM Oct 26th, 3:00 PM

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.