Evidence map›Paper›PMID 23298809›Full record

ArticleBioorganic & medicinal chemistry letters2013

Optimization of benzyloxazoles as non-nucleoside inhibitors of HIV-1 reverse transcriptase to enhance Y181C potency.

Mariela Bollini, Ricardo Gallardo-Macias, Krasimir A Spasov, Julian Tirado-Rives, Karen S Anderson, William L Jorgensen

Abstract read
In one paragraph

Article in Bioorganic & medicinal chemistry letters, 2013. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 7 papers.

0numbers the graph read from it
0cells of the map it votes in
7citing papers in PubMed
–field-weighted citation impact
1 · What the graph read from it

What it found

Each row is one number read from the abstract, on the scale the paper reported it, with its interval. Left of the dashed line favours the treatment, right favours the comparator. Under each row is the sentence it came from. New to these charts? A ten-minute tutorial.

The abstract states no effect estimate the extractor could read, or names no intervention and outcome on the map, so this paper lights no cell and moves no belief. It is still indexed, cited and linked below.

2 · The registry

The trial behind it

Trials whose registry record cites this paper, or whose number appears in the abstract. A trial that started after this paper was published is citing it as background, not reporting it.

Neither the registry nor the abstract names a trial number. If this is a trial report, that itself is worth knowing.

3 · Its place in the literature

Who cites it

7 citing papers in PubMed.

  1. Article
  2. Article
  3. Covalent inhibitors for eradication of drug-resistant HIV-1 reverse transcriptase: From design to protein crystallography.Proceedings of the National Academy of Sciences of the United States of America · 2017
    Article
  4. Article
  5. Computer-aided discovery of anti-HIV agents.Bioorganic & medicinal chemistry · 2016
    Article
  6. Article
  7. Article
4 · The record

Corrections and comments

PubMed lists nothing against this paper. Absence here is not a guarantee, only a check that was made.

5 · Who and what money

Authors and funding

6 authors.

Mariela BolliniDepartment of Chemistry, Yale University, New Haven, CT 06520-8107, USA.
Ricardo Gallardo-Macias
Krasimir A Spasov
Julian Tirado-Rives
Karen S Anderson
William L Jorgensen

Funding

MECHANISM AND INHIBITION OF HIV REVERSE TRANSCRIPTASER01GM049551 · NIGMS · YALE UNIVERSITY · PI ANDERSON, KAREN S. · 1993 to 2019
$9.0M
POTENTIAL FUNCTIONS FOR WATER PROTEIN INTERACTIONSR01GM032136 · NIGMS · YALE UNIVERSITY · PI JORGENSEN, WILLIAM L. · 1985 to 2023
$8.2M
COMPUTER-AIDED DESIGN OF ANTIHIV DRUGSR01AI044616 · NIAID · YALE UNIVERSITY · PI JORGENSEN, WILLIAM L. · 1999 to 2022
$7.7M
NIAID NIH HHS AI44616NIAID NIH HHS R01 AI044616NIGMS NIH HHS GM32136NIGMS NIH HHS GM49551NIGMS NIH HHS R01 GM032136NIGMS NIH HHS R01 GM049551
6 · The paper itself

Abstract

Design of non-nucleoside inhibitors of HIV-1 reverse transcriptase with improved activity towards Tyr181Cys containing variants was pursued with the assistance of free energy perturbation (FEP) calculations. Optimization of the 4-R substituent in 1 led to ethyl and isopropyl analogs 1e and 1f with 1-7 nM potency towards both the wild-type virus and a Tyr181C variant.

Indexed as

Anti-HIV AgentsDrug DesignHIV-1HIV Reverse TranscriptaseHumansModels, MolecularReverse Transcriptase InhibitorsStructure-Activity RelationshipAnti-HIV AgentsHIV Reverse TranscriptaseReverse Transcriptase Inhibitors

Identifiers

PMID23298809
PMCPMC3561933

What OpenQuestion holds

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Registered trials

None linked

Read under generation 80e0d062 · epoch 390. Bibliography from PubMed, PubMed Central and OpenAlex; grants from NIH RePORTER; trial links from ClinicalTrials.gov; estimates, votes and beliefs from the OpenQuestion graph.