Design and synthesis of peptide-based macrocyclic cyclophilin inhibitors.

The efficient assembly of an 18-membered macrocyclic peptide core was realized by a straightforward and convergent approach utilizing ring-closing metathesis of the corresponding linear tetrapeptides as the key transformation. This approach allowed for the facile preparation of a focused library of novel macrocycles that culminated in the discovery of a cyclophilin A inhibitor with a Kd=5.4μM. Copyright © 2016 Elsevier Ltd. All rights reserved.

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Brett A Granger, Dean G Brown. Design and synthesis of peptide-based macrocyclic cyclophilin inhibitors. Bioorganic & medicinal chemistry letters. 2016 Nov 01;26(21):5304-5307

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PMID: 27687672

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