Potent selective thienoxazinone inhibitors of herpes proteases

RL Jarvest, SC Connor, JG Gorniak, LJ Jennings…

Index: Jarvest, Richard L.; Connor, Susan C.; Gorniak, Joselina G.; Jennings, L. John; Serafinowska, Halina T.; West, Andrew Bioorganic and Medicinal Chemistry Letters, 1997 , vol. 7, # 13 p. 1733 - 1738

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Citation Number: 45

Abstract

Thieno [3, 2-d] oxazinones are potent, selective, mechanism-based inhibitors of the herpes proteases with good aqueous stability. Specificity between the HSV and CMV proteases varies across the series: compounds 14b and 14c are submicromolar HSV protease inhibitors with modest CMV protease inhibition, 14g is a selective CMV protease inhibitor; and 32 inhibits both enzymes with an IC50 of about 1 μM.