当前位置： SCI文献检索 > JOURNAL OF MEDICINAL CHEMISTRY期刊下所有文献 > 5,6,7,8-Tetrahydro-1,6-naphthyridine Derivatives as Potent HIV-1-Integrase-Allosteric-Site Inhibitors.

5,6,7,8-Tetrahydro-1,6-naphthyridine Derivatives as Potent HIV-1-Integrase-Allosteric-Site Inhibitors.

Abstract：

:A series of 5,6,7,8-tetrahydro-1,6-naphthyridine derivatives targeting the allosteric lens-epithelium-derived-growth-factor-p75 (LEDGF/p75)-binding site on HIV-1 integrase, an attractive target for antiviral chemotherapy, was prepared and screened for activity against HIV-1 infection in cell culture. Small molecules that bind within the LEDGF/p75-binding site promote aberrant multimerization of the integrase enzyme and are of significant interest as HIV-1-replication inhibitors. Structure-activity-relationship studies and rat pharmacokinetic studies of lead compounds are presented.

journal_name

J Med Chem

journal_title

Journal of medicinal chemistry

authors

Peese KM,Allard CW,Connolly T,Johnson BL,Li C,Patel M,Sorensen ME,Walker MA,Meanwell NA,McAuliffe B,Minassian B,Krystal M,Parker DD,Lewis HA,Kish K,Zhang P,Nolte RT,Simmermacher J,Jenkins S,Cianci C,Naidu BN

doi

10.1021/acs.jmedchem.8b01473

subject

Has Abstract

pub_date

2019-02-14 00:00:00

pages

1348-1361

issue

3

eissn

0022-2623

issn

1520-4804

journal_volume

62

pub_type

杂志文章

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