Evidence map›Paper›PMID 31416666›Full record

ArticleBioorganic & medicinal chemistry letters2019

Potent HIV-1 protease inhibitors incorporating squaramide-derived P2 ligands: Design, synthesis, and biological evaluation.

Arun K Ghosh, Jacqueline N Williams, Satish Kovela, Jun Takayama, Hannah M Simpson, D Eric Walters, Shin-Ichiro Hattori, Manabu Aoki, Hiroaki Mitsuya

Abstract read
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In one paragraph

Article in Bioorganic & medicinal chemistry letters, 2019. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 2 papers.

0numbers the graph read from it
0cells of the map it votes in
2citing 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

2 citing papers in PubMed.

  1. Article
  2. 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

9 authors.

Arun K GhoshDepartment of Chemistry, Purdue University, West Lafayette, IN 47907, USA; Department of Medicinal Chemistry, Purdue University, West Lafayette, IN 47907, USA. Electronic address: akghosh@purdue.edu.
Jacqueline N WilliamsDepartment of Chemistry, Purdue University, West Lafayette, IN 47907, USA; Department of Medicinal Chemistry, Purdue University, West Lafayette, IN 47907, USA.
Satish KovelaDepartment of Chemistry, Purdue University, West Lafayette, IN 47907, USA; Department of Medicinal Chemistry, Purdue University, West Lafayette, IN 47907, USA.
Jun TakayamaDepartment of Chemistry, Purdue University, West Lafayette, IN 47907, USA; Department of Medicinal Chemistry, Purdue University, West Lafayette, IN 47907, USA.
Hannah M SimpsonDepartment of Chemistry, Purdue University, West Lafayette, IN 47907, USA; Department of Medicinal Chemistry, Purdue University, West Lafayette, IN 47907, USA.
D Eric WaltersDepartment of Pharmaceutical Sciences, Rosalind Franklin University of Medicine and Science, North Chicago, IL 60064, USA.
Shin-Ichiro HattoriDepartment of Refractory Viral Infections, National Center for Global Health and Medicine, Shinjuku, Tokyo 162-8655, Japan.
Manabu AokiDepartment of Refractory Viral Infections, National Center for Global Health and Medicine, Shinjuku, Tokyo 162-8655, Japan; Experimental Retrovirology Section, HIV and AIDS Malignancy Branch National Cancer Institute, Bethesda, MD 20892, USA.
Hiroaki MitsuyaDepartment of Refractory Viral Infections, National Center for Global Health and Medicine, Shinjuku, Tokyo 162-8655, Japan; Experimental Retrovirology Section, HIV and AIDS Malignancy Branch National Cancer Institute, Bethesda, MD 20892, USA; Division of Clinical Sciences, Kumamoto University Hospital, Kumamoto 860-8556, Japan.

Funding

Design & Synthesis of Nonpeptide Protease InhibitorsR37GM053386 · NIGMS · PURDUE UNIVERSITY · PI GHOSH, ARUN K · 2011 to 2018
$3.9M
DESIGN AND SYNTHESIS OF NONPEPTIDE PROTEASE INHIBITORSR01GM053386 · NIGMS · UNIVERSITY OF ILLINOIS AT CHICAGO · PI GHOSH, ARUN K · 1995 to 2010
$3.7M
Design & Synthesis of Nonpeptide Protease InhibitorsR37AI150466 · NIAID · PURDUE UNIVERSITY · PI GHOSH, ARUN K · 2019 to 2020
$969k
NIAID NIH HHS R37 AI150466NIGMS NIH HHS R01 GM053386NIGMS NIH HHS R37 GM053386
6 · The paper itself

Abstract

We describe the design, synthesis, and biological evaluation of novel HIV-1 protease inhibitors containing a squaramide-derived scaffold as the P2 ligand in combination with a (R)-hydroxyethylamine sulfonamide isostere. Inhibitor 3h with an N-methyl-3-(R)-aminotetrahydrofuranyl squaramide P2-ligand displayed an HIV-1 protease inhibitory K

Indexed as

Drug DesignDose-Response Relationship, DrugEthers, CyclicHIV ProteaseHIV Protease InhibitorsHumansLigandsMolecular StructureQuinineStructure-Activity RelationshipEthers, CyclicHIV ProteaseHIV Protease InhibitorsLigandsp16 protease, Human immunodeficiency virus 1QuininesquaramideBis-tetrahydrofuranHIV-1 proteaseInhibitorSquaramideSynthesis

Identifiers

PMID31416666
PMCPMC6711809

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Registered trials

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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.