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Structure-based design and synthesis of macrocyclic human rhinovirus 3C protease inhibitors.

Abstract：

:The design and synthesis of macrocyclic inhibitors of human rhinovirus 3C protease is described. A macrocyclic linkage of the P1 and P3 residues, and the subsequent structure-based optimization of the macrocycle conformation and size led to the identification of a potent biochemical inhibitor 10 with sub-micromolar antiviral activity.

journal_name

Bioorg Med Chem Lett

journal_title

Bioorganic & medicinal chemistry letters

authors

Namoto K,Sirockin F,Sellner H,Wiesmann C,Villard F,Moreau RJ,Valeur E,Paulding SC,Schleeger S,Schipp K,Loup J,Andrews L,Swale R,Robinson M,Farady CJ

doi

10.1016/j.bmcl.2018.01.064

subject

Has Abstract

pub_date

2018-03-01 00:00:00

pages

906-909

issue

5

eissn

0960-894X

issn

1464-3405

pii

S0960-894X(18)30075-1

journal_volume

28

pub_type

杂志文章

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