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3-Hydroxy-1,5-dihydro-pyrrol-2-one derivatives as advanced inhibitors of HIV integrase.

Abstract：

:The two-metal binding model we previously reported as an inhibition mechanism of HIV integrase (HIV IN) produced a new direction in modification of 2-hydroxy-3-heteroaryl acrylic acid inhibitors (HHAAs). Here we present a novel series of HIV IN inhibitors having a 3-hydroxy-1,5-dihydro-pyrrol-2-one moiety (HDPO) as an advanced analog of HHAAs. This cyclic modification of the chelating region of HHAA produces a favorable configuration to coordinate two-metal ions in HIV IN, which consequently gave improvements in not only enzymatic assay but also antiviral cell based assay in many cases.

journal_name

Bioorg Med Chem

journal_title

Bioorganic & medicinal chemistry

authors

Kawasuji T,Fuji M,Yoshinaga T,Sato A,Fujiwara T,Kiyama R

doi

10.1016/j.bmc.2007.05.052

subject

Has Abstract

pub_date

2007-08-15 00:00:00

pages

5487-92

issue

16

eissn

0968-0896

issn

1464-3391

pii

S0968-0896(07)00468-3

journal_volume

15

pub_type

杂志文章

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