Author/Authors :
James J. -W. Duan، نويسنده , , Lihua Chen، نويسنده , , Chu-Biao Xue، نويسنده , , Zelda R. Wasserman، نويسنده , , Karl D. Hardman، نويسنده , , Maryanne B. Covington، نويسنده , , Robert R. Cope، نويسنده , , Elizabeth C. Arner، نويسنده , , Carl P. Decicco، نويسنده ,
Abstract :
A novel series of 13- and 14-membered macrocyclic amines was developed by linking the P1 and P2′ groups. The synthesis entails stereoselective Frater alkylation to install the anti-succinate configuration and macrocyclic amination via nucleophilic displacement. This strategy resulted in a new class of conformationally constrained inhibitors that are potent and selective for MMP-8 and 9 over MMP-1 and 3.
