Evidence map›Paper›PMID 31549492›Full record

ArticleChemMedChem2019

Potent HIV-1 Protease Inhibitors Containing Carboxylic and Boronic Acids: Effect on Enzyme Inhibition and Antiviral Activity and Protein-Ligand X-ray Structural Studies.

Arun K Ghosh, Zilei Xia, Satish Kovela, William L Robinson, Megan E Johnson, Daniel W Kneller, Yuan-Fang Wang, Manabu Aoki, Yuki Takamatsu, Irene T Weber and 1 more

Open access · greenAbstract read
In one paragraph

Article in ChemMedChem, 2019. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 12 papers.

0numbers the graph read from it
0cells of the map it votes in
12citing papers in PubMed
1.9field-weighted citation impact, top 15% of its field
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

12 citing papers in PubMed, 26 citations in OpenAlex.

  1. Fused 3D boron heterocyclesChemical science · 2026
    Article
  2. Recent Advances in Heterocyclic HIV Protease Inhibitors.International journal of molecular sciences · 2025
    Review
  3. Review
  4. Review
  5. Article
  6. Article
  7. Article
  8. Article
  9. Article
  10. Review
  11. Merging the Versatile Functionalities of Boronic Acid with Peptides.International journal of molecular sciences · 2021
    Review
  12. Review
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

11 authors at 3 institutions in 2 countries.

Arun K GhoshDepartment of Chemistry and Department of Medicinal Chemistry, Purdue University, West Lafayette, IN, 47907, USA.ORCID 0000-0003-2472-1841
Zilei XiaDepartment of Chemistry and Department of Medicinal Chemistry, Purdue University, West Lafayette, IN, 47907, USA.
Satish KovelaDepartment of Chemistry and Department of Medicinal Chemistry, Purdue University, West Lafayette, IN, 47907, USA.
William L RobinsonDepartment of Chemistry and Department of Medicinal Chemistry, Purdue University, West Lafayette, IN, 47907, USA.
Megan E JohnsonDepartment of Chemistry and Department of Medicinal Chemistry, Purdue University, West Lafayette, IN, 47907, USA.
Daniel W KnellerDepartments of Biology and Chemistry, Molecular Basis of Disease, Georgia State University, Atlanta, GA, 30303, USA.
Yuan-Fang WangDepartments of Biology and Chemistry, Molecular Basis of Disease, Georgia State University, Atlanta, GA, 30303, USA.
Manabu AokiExperimental Retrovirology Section, HIV and AIDS Malignancy Branch, National Cancer Institute, Bethesda, MD, 20892, USA.
Yuki TakamatsuDepartment of Refractory Viral Infections, National Center for Global Heath and Medicine Research Institute, Shinjuku, Tokyo, 162-8655, Japan.
Irene T WeberDepartments of Biology and Chemistry, Molecular Basis of Disease, Georgia State University, Atlanta, GA, 30303, USA.
Hiroaki MitsuyaDepartments of Hematology and Infectious Diseases, Kumamoto University School of Medicine, Kumamoto, 860-8556, Japan.
Purdue University West Lafayette · USGeorgia State University · USNational Center for Global Health and Medicine · JP

Funding

Taking aim at HBV eradication using novel NRTIs and Capsid effectorsR01AI121315 · NIAID · UNIVERSITY OF MISSOURI-COLUMBIA · PI SARAFIANOS, STEFAN G, WANG, ZHENGQIANG · 2016 to 2020
$3.0M
Design & Synthesis of Nonpeptide Protease InhibitorsR01AI150466 · NIAID · PURDUE UNIVERSITY · PI ARUN K GHOSH · 2023 to 2026
$2.4M
Design & Synthesis of Nonpeptide Protease InhibitorsR37AI150466 · NIAID · PURDUE UNIVERSITY · PI GHOSH, ARUN K · 2019 to 2020
$969k
Inhibition of Resistant Variants of HIV ProteaseU01AI150461 · NIAID · GEORGIA STATE UNIVERSITY · PI HARRISON, ROBERT WILSON, WEBER, IRENE T · 2019 to 2020
$691k
NIAID NIH HHS R01 AI121315NIAID NIH HHS R01 AI150466NIAID NIH HHS R37 AI150466NIAID NIH HHS U01 AI150461NIH HHS AI150461NIH HHS AI150466
6 · The paper itself

Abstract

We report the synthesis and biological evaluation of phenylcarboxylic acid and phenylboronic acid containing HIV-1 protease inhibitors and their functional effect on enzyme inhibition and antiviral activity in MT-2 cell lines. Inhibitors bearing bis-THF ligand as P2 ligand and phenylcarboxylic acids and carboxamide as the P2' ligands, showed very potent HIV-1 protease inhibitory activity. However, carboxylic acid containing inhibitors showed very poor antiviral activity relative to carboxamide-derived inhibitors which showed good antiviral IC

Indexed as

Anti-HIV AgentsBoronic AcidsCarboxylic AcidsCell LineCrystallography, X-RayHIV-1HIV ProteaseHIV Protease InhibitorsHumansLigandsModels, MolecularMolecular ConformationAnti-HIV AgentsBoronic AcidsCarboxylic AcidsHIV ProteaseHIV Protease InhibitorsLigandsp16 protease, Human immunodeficiency virus 1brain penetrationdrug resistancegenetic barriersHIV-1 protease inhibitorsstructure-based design

Identifiers

PMID31549492
PMCPMC6842059
OpenAlexW2976127408

What OpenQuestion holds

Textmetadata
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Read underepoch 390

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.