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Substituted naphthalenones as a new structural class of HIV-1 reverse transcriptase inhibitors.

Abstract：

:A novel substituted naphthalenone (TGG-II-23A) has been found that inhibits HIV-1 infection of CEM-SS cells at concentrations that are not cytotoxic. Time of addition experiments indicate that TGG-II-23A functions at a stage of the HIV-1 life cycle at or near reverse transcription. Cell free assays confirmed that TGG-II-23A inhibits HIV-1 reverse transcriptase. Similar to other non-nucleoside inhibitors, TGG-II-23A was specific for HIV-1 and failed to inhibit the replication of HIV-2. The binding site of TGG-II-23A appears to be in close proximity to that of the TIBO-like inhibitors, since a TIBO-resistant HIV-1 was also resistant to TGG-II-23A treatment. TGG-II-23A is a mixed non-competitive inhibitor that exhibits the same template:primer selectivity as other non-nucleoside inhibitors. TGG-II-23A therefore represents a new structural entry into the TIBO/Nevirapine class of inhibitors of HIV-1 reverse transcriptase.

journal_name

Antiviral Res

journal_title

Antiviral research

authors

Alam M,Bechtold CM,Patick AK,Skoog MT,Gant TG,Colonno RJ,Meyers AI,Li H,Trimble J,Lin PF

doi

10.1016/0166-3542(93)90091-v

subject

Has Abstract

pub_date

1993-10-01 00:00:00

pages

131-41

issue

2-3

eissn

0166-3542

issn

1872-9096

pii

0166-3542(93)90091-V

journal_volume

22

pub_type

杂志文章

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