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P3-P4 ureas and reverse carbamates as potent HCV NS3 protease inhibitors: Effective transposition of the P4 hydrogen bond donor.

Abstract：

:A series of tripeptidic acylsulfonamide inhibitors of HCV NS3 protease were prepared that explored structure-activity relationships (SARs) at the P4 position, and their in vitro and in vivo properties were evaluated. Enhanced potency was observed in a series of P4 ureas; however, the PK profiles of these analogues were less than optimal. In an effort to overcome the PK shortcomings, modifications to the P3-P4 junction were made. This included a strategy in which one of the two urea N-H groups was either N-methylated or replaced with an oxygen atom. The former approach provided a series of regioisomeric N-methylated ureas while the latter gave rise to P4 reverse carbamates, both of which retained potent NS3 inhibitory properties while relying upon an alternative H-bond donor topology. Details of the SARs and PK profiles of these analogues are provided.

journal_name

Bioorg Med Chem Lett

journal_title

Bioorganic & medicinal chemistry letters

authors

Venables BL,Sin N,Wang AX,Sun LQ,Tu Y,Hernandez D,Sheaffer A,Lee M,Dunaj C,Zhai G,Barry D,Friborg J,Yu F,Knipe J,Sandquist J,Falk P,Parker D,Good AC,Rajamani R,McPhee F,Meanwell NA,Scola PM

doi

10.1016/j.bmcl.2018.04.009

subject

Has Abstract

pub_date

2018-06-01 00:00:00

pages

1853-1859

issue

10

eissn

0960-894X

issn

1464-3405

pii

S0960-894X(18)30307-X

journal_volume

28

pub_type

杂志文章

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