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Bismacrocyclic Inhibitors of Hepatitis C NS3/4a Protease
Author(s) -
McCauley John A.,
Rudd Michael T.,
Nguyen Kevin T.,
McIntyre Charles J.,
Romano Joseph J.,
Bush Kimberly J.,
Varga Sandor L.,
Ross Charles W.,
Carroll Steven S.,
DiMuzio Jillian,
Stahlhut Mark W.,
Olsen David B.,
Lyle Terry A.,
Vacca Joseph P.,
Liverton Nigel J.
Publication year - 2008
Publication title -
angewandte chemie international edition
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 5.831
H-Index - 550
eISSN - 1521-3773
pISSN - 1433-7851
DOI - 10.1002/anie.200803298
Subject(s) - ring closing metathesis , protease , closing (real estate) , ns3 , derivative (finance) , metathesis , stereochemistry , information retrieval , salt metathesis reaction , potency , virology , computer science , chemistry , combinatorial chemistry , medicine , biochemistry , organic chemistry , political science , business , enzyme , law , finance , polymerization , polymer , in vitro
Double time : The bismacrocycle 2 was prepared from 1 by a selective double ring‐closing metathesis (RCM) reaction to form the 18‐ and 15‐membered rings simultaneously. Derivative 3 shows excellent potency against NS3/4a protease.