Novel Peptidomimetic Hepatitis C Virus NS3/4A Protease Inhibitors Spanning the P2–P1′ Region

…, UH Danielson, A Karlén, A Sandström

Index: Lampa, Anna K.; Bergman, Sara M.; Gustafsson, Sofia S.; Alogheli, Hiba; Akerblom, Eva B.; Lindeberg, Gunnar G.; Svensson, Richard M.; Artursson, Per; Danielson, U. Helena; Karlen, Anders; Sandstroem, Anja ACS Medicinal Chemistry Letters, 2014 , vol. 5, # 3 p. 249 - 254

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Citation Number: 6

Abstract

Herein, novel hepatitis C virus NS3/4A protease inhibitors based on a P2 pyrimidinyloxyphenylglycine in combination with various regioisomers of an aryl acyl sulfonamide functionality in P1 are presented. The P1′ 4-(trifluoromethyl) phenyl side chain was shown to be particularly beneficial in terms of inhibitory potency. Several inhibitors with K i-values in the nanomolar range were developed and included identification of ...