Evidence map›Paper›PMID 30354121›Full record

ArticleJournal of medicinal chemistry2018

Design and Synthesis of Potent HIV-1 Protease Inhibitors Containing Bicyclic Oxazolidinone Scaffold as the P2 Ligands: Structure-Activity Studies and Biological and X-ray Structural Studies.

Arun K Ghosh, Jacqueline N Williams, Rachel Y Ho, Hannah M Simpson, Shin-Ichiro Hattori, Hironori Hayashi, Johnson Agniswamy, Yuan-Fang Wang, Irene T Weber, Hiroaki Mitsuya

Open access · greenAbstract read
In one paragraph

Article in Journal of medicinal chemistry, 2018. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 8 papers.

0numbers the graph read from it
0cells of the map it votes in
8citing 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

8 citing papers in PubMed, 12 citations in OpenAlex.

  1. Review
  2. Review
  3. Article
  4. The Pseudo-SymmetricBiomolecules · 2021
    Article
  5. Article
  6. Article
  7. Inhibition of HIV-1 Protease byEvidence-based complementary and alternative medicine : eCAM · 2020
    Article
  8. 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

10 authors at 1 institution in 1 country.

Arun K GhoshDepartment of Chemistry and Department of Medicinal Chemistry , Purdue University , 560 Oval Drive , West Lafayette , Indiana 47907 , United States.ORCID 0000-0003-2472-1841
Jacqueline N WilliamsDepartment of Chemistry and Department of Medicinal Chemistry , Purdue University , 560 Oval Drive , West Lafayette , Indiana 47907 , United States.
Rachel Y HoDepartment of Chemistry and Department of Medicinal Chemistry , Purdue University , 560 Oval Drive , West Lafayette , Indiana 47907 , United States.
Hannah M SimpsonDepartment of Chemistry and Department of Medicinal Chemistry , Purdue University , 560 Oval Drive , West Lafayette , Indiana 47907 , United States.
Shin-Ichiro HattoriDepartment of Refractory Viral Infections , National Center for Global Health and Medicine Research Institute , Tokyo 162-8655 , Japan.
Hironori HayashiDepartment of Refractory Viral Infections , National Center for Global Health and Medicine Research Institute , Tokyo 162-8655 , Japan.
Johnson AgniswamyDepartment of Biology, Molecular Basis of Disease , Georgia State University , Atlanta , Georgia 30303 , United States.
Yuan-Fang WangDepartment of Biology, Molecular Basis of Disease , Georgia State University , Atlanta , Georgia 30303 , United States.
Irene T WeberDepartment of Biology, Molecular Basis of Disease , Georgia State University , Atlanta , Georgia 30303 , United States.ORCID 0000-0003-4876-7393
Hiroaki MitsuyaDepartment of Refractory Viral Infections , National Center for Global Health and Medicine Research Institute , Tokyo 162-8655 , Japan.
Purdue University West Lafayette · US

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
ACTIVITY OF RESISTANT VARIANTS OF HIV PROTEASER01GM062920 · NIGMS · GEORGIA STATE UNIVERSITY · PI WEBER, IRENE T · 2000 to 2012
$3.3M
Inhibition of Resistant Variants of HIV ProteaseU01GM062920 · NIGMS · GEORGIA STATE UNIVERSITY · PI HARRISON, ROBERT WILSON, WEBER, IRENE T · 2013 to 2018
$2.1M
Structural Analysis of Antiviral Activity of Novel Agents against HIVZIABC011880 · NCI · DIVISION OF BASIC SCIENCES - NCI · PI MITSUYA, HIROAKI · 2019 to 2019
$250k
NIGMS NIH HHS R01 GM053386NIGMS NIH HHS R01 GM062920NIGMS NIH HHS R37 GM053386NIGMS NIH HHS U01 GM062920
6 · The paper itself

Abstract

We have designed, synthesized, and evaluated a new class of potent HIV-1 protease inhibitors with novel bicyclic oxazolidinone derivatives as the P2 ligand. We have developed an enantioselective synthesis of these bicyclic oxazolidinones utilizing a key o-iodoxybenzoic acid mediated cyclization. Several inhibitors displayed good to excellent activity toward HIV-1 protease and significant antiviral activity in MT-4 cells. Compound 4k has shown an enzyme K

Indexed as

Drug DesignCatalytic DomainChemistry Techniques, SyntheticHIV-1HIV ProteaseHIV Protease InhibitorsLigandsModels, MolecularOxazolidinonesStereoisomerismStructure-Activity RelationshipHIV ProteaseHIV Protease InhibitorsLigandsOxazolidinones

Identifiers

PMID30354121
PMCPMC6541917
OpenAlexW2898459924

What OpenQuestion holds

Textmetadata
LicenceTDM
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.