当前位置： SCI文献检索 > EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY期刊下所有文献 > The design of 8-hydroxyquinoline tetracyclic lactams as HIV-1 integrase strand transfer inhibitors.

The design of 8-hydroxyquinoline tetracyclic lactams as HIV-1 integrase strand transfer inhibitors.

Abstract：

:A novel series of HIV-1 integrase strand transfer inhibitors were designed using the venerable two-metal binding pharmacophore model and incorporating structural elements from two different literature scaffolds. This manuscript describes a number of 8-hydroxyquinoline tetracyclic lactams with exceptional antiviral activity against HIV-1 and little loss of potency against the IN signature resistance mutations Q148K and G140S/Q148H.

journal_name

Eur J Med Chem

journal_title

European journal of medicinal chemistry

authors

Velthuisen EJ,Johns BA,Temelkoff DP,Brown KW,Danehower SC

doi

10.1016/j.ejmech.2016.03.038

subject

Has Abstract

pub_date

2016-07-19 00:00:00

pages

99-112

eissn

0223-5234

issn

1768-3254

pii

S0223-5234(16)30212-4

journal_volume

117

pub_type

杂志文章

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