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公开(公告)号：US11713339B2
公开(公告)日：2023-08-01
申请号：US17042489
申请日：2019-03-28
Applicant: UNIVERSITY OF WARWICK
Inventor： Michael Shipman
CPC classification number: C07K7/54 , G01N33/6803 , A61K38/00
Abstract: A method of macrocyclization of peptidomimetics is described which comprises substitution of one or more of the backbone amide C═O bonds with a turn-inducing motif. The method is general with enhancements seen across a range of ring sizes (e.g. tri-, tetra-, penta- and hexapeptides). Specifically, a peptidomimetic macrocycle is described comprising a carbonyl bioisosteric turn-inducing element having the structure:
wherein X is a heteroatom; and
wherein R1 to R6 are each independently selected from alkyl, aryl, heteroaryl and H.
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