Bioorganic and Medicinal Chemistry Letters p. 1453 - 1458 (1999)
Update date:2022-08-04
Topics:
Duan, James J.-W
Chen, Lihua
Xue, Chu-Biao
Wasserman, Zelda R.
Hardman, Karl D.
Covington, Maryanne B.
Copeland, Robert R.
Arner, Elizabeth C.
Decicco, Carl P.
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.
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