Author/Authors :
Dashyant Dhanak، نويسنده , , Richard M. Keenan، نويسنده , , George Burton، نويسنده , , Arun Kaura، نويسنده , , Michael G. Darcy، نويسنده , , Dinubhai H. Shah، نويسنده , , Lance H. Ridgers، نويسنده , , Ann Breen، نويسنده , , Paddy Lavery، نويسنده , , David G. Tew، نويسنده , , Andrew-West، نويسنده ,
Abstract :
A novel class of CMV protease inhibitors based on a benzothiopyran-S,S-dioxide nucleus has been discovered. Enzyme kinetic data supports a reversible mode of inhibition for a representative member of this class, 2-(3-pyridyl-N-oxide)benzothiopyran-4-one-S,S-dioxide, 1. Experiments in the presence and absence of the disulfide reducing agent DTT suggest that the inhibition by 1 is not due to oxidative inactivation of the enzyme. Also presented are results of some SAR studies of the benzothiopyranone ring system.