Discover Community Create You

Loading publication...

Noodle always counts identifier-free feature events for service operation. With your permission, Google Analytics can also estimate audience and engagement. Search text, publication identifiers, cookies, IP addresses and browser fingerprints are never included in Noodle's first-party event counters.

Privacy details

Article

Discovery of potent HIV integrase inhibitors active against raltegravir resistant viruses.

Bioorganic & medicinal chemistry letters - 1 Sept 2010

Le Giang, Vandegraaff Nick, Rhodes David I, Jones Eric D, Coates Jonathan A V, Lu Long, Li Xinming, Yu Changjiang, Feng Xiao, Deadman John J

Abstract excerpt

A series of novel HIV integrase inhibitors active against rategravir resistant strains are reported. Initial SAR studies revealed that activities against wild-type virus were successfully maintained at single digit nanomolar level with a wide range of substitutions. However, inclusion of nitrogen-based cyclic substitutions was crucial for achieving potency against mutant viruses. Several compounds with excellent...

Read the complete abstract on PubMed

Topics

Share this publication in a Topic to start or enrich a Post.

Share to Drug Discovery
Share to Drug Resistance, Viral

Methodology Data sources Editorial policy Privacy About Contact Helena Bioinformatics

Share to HIV Integrase Inhibitors

Share to Mutation

Share to Pyrrolidinones

Share to Raltegravir Potassium

Share to Structure-Activity Relationship

Source

Identifiers

PMID: 20685117
DOI: 10.1016/j.bmcl.2010.07.041

Provenance

PubMed metadata and Literature Corpus relationships. Corpus snapshot updated 7 Sept 2026. Manifest publication-graph-cohort-2026-09-07.1.

Source receipt: pubmed, retrieved 7 Sept 2026.

Related research

Semantic proximity does not establish scientific evidence.

Research trail→

Click a neighbor to travelStep 1 · 12 closest

Discovery of potent HIV integrase inhibitors active against raltegravir resistant viruses.PMID 20685117Read ↗

Overcoming HIV drug resistance through rational drug design based on molecular, biochemical, and structural profiles of HIV resistance.Semantic proximity Read ↗

Development of enhanced HIV-1 non-nucleoside reverse transcriptase inhibitors with improved resistance and pharmacokinetic profiles.Semantic proximity Read ↗

Non-Nucleoside Reverse Transcriptase Inhibitors Join Forces with Integrase Inhibitors to Combat HIVSemantic proximity Read ↗

Avoiding Drug Resistance in HIV Reverse Transcriptase.Semantic proximity Read ↗

Design and synthesis of highly potent HIV protease inhibitors with activity against resistant virus.Semantic proximity Read ↗

The Current Status of the NNRTI Family of Antiretrovirals Used Against HIV InfectionSemantic proximity Read ↗

Structure, Synthesis and Inhibition Mechanism of Nucleoside Analogues as HIV‐1 Reverse Transcriptase Inhibitors (NRTIs)Semantic proximity Read ↗

Spectrum of Activity of Raltegravir and Dolutegravir Against Novel Treatment-Associated Mutations in HIV-2 Integrase: A Phenotypic Analysis Using an Expanded Panel of Site-Directed Mutants.Semantic proximity Read ↗

4-amino-1-hydroxy-2-oxo-1,8-naphthyridine-containing compounds having high potency against raltegravir-resistant integrase mutants of HIV-1.Semantic proximity Read ↗

Integrase inhibitors in the treatment of HIV-1 infectionSemantic proximity Read ↗

Recent advances in the discovery and development of novel HIV-1 NNRTI platforms: 2006-2008 update.Semantic proximity Read ↗

Structural basis for drug resistance mechanisms for non-nucleoside inhibitors of HIV reverse transcriptaseSemantic proximity Read ↗

⌁Select a neighboring publication to make it the new centre.