1-Aminocyclopropaneboronic acid: synthesis and incorporation into an inhibitor of hepatitis C virus NS3 protease |
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Authors: | Priestley E S Decicco C P |
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Affiliation: | Department of Chemical and Physical Sciences, DuPont Pharmaceuticals Company, P.O. Box 80500, Wilmington, Delaware 19880, USA. e.scott.priestley@dupontpharma.com |
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Abstract: | The previously unreported alpha,alpha-disubstituted 1-aminoboronate esters have potential utility in peptidomimetic design, particularly against serine protease targets. A concise synthesis of 1-aminocyclopropaneboronate pinanediol ester is reported, and a peptidyl derivative is shown to have modest affinity (K(i) = 1.6 microM) for hepatitis C NS3 protease. |
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