Optimizing the metabolic stability of an antitubercular
What is it about?
A thienopyrimidine antitubercular was found to be metabolically unstable in mouse liver microsomes in vitro. Steps were taken to modify the molecule that was chemocentric and involved understanding the metabolic fate of the initial hit in vitro.
Why is it important?
Mouse metabolic stability is an important ADME property which can determine whether an antitubercular has in vivo efficacy in the mouse. Therefore modifying the structure to maintain the in vitro activity and improve the metabolic stability is a challenge.
The following have contributed to this page: Dr Sean Ekins