Evidence map›Paper›PMID 21428405›Full record

ArticleJournal of medicinal chemistry2011

Chemistry and biology of macrolide antiparasitic agents.

Younjoo Lee, Jun Yong Choi, Hong Fu, Colin Harvey, Sandeep Ravindran, William R Roush, John C Boothroyd, Chaitan Khosla

Open access · greenAbstract read
In one paragraph

Article in Journal of medicinal chemistry, 2011. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 15 papers.

0numbers the graph read from it
0cells of the map it votes in
15citing papers in PubMed
1.2field-weighted citation impact, top 25% 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

15 citing papers in PubMed, 44 citations in OpenAlex.

  1. Article
  2. Article
  3. Article
  4. Article
  5. Review
  6. Targeting malaria parasites with novel derivatives of azithromycin.Frontiers in cellular and infection microbiology · 2022
    Article
  7. Multipurpose Drugs Active Against BothFrontiers in cellular and infection microbiology · 2021
    Review
  8. Article
  9. Article
  10. Review
  11. Article
  12. Article
  13. Article
  14. Chemobiosynthesis of new antimalarial macrolides.Antimicrobial agents and chemotherapy · 2013
    Article
  15. 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

8 authors at 3 institutions in 1 country.

Younjoo LeeDepartment of Chemistry, Stanford University, Stanford, California 94305, United States.
Jun Yong Choi
Hong Fu
Colin Harvey
Sandeep Ravindran
William R Roush
John C Boothroyd
Chaitan Khosla
Scripps Research Institute · USScripps (United States) · USStanford University · US

Funding

Scripps Research Institute Molecular Screen Center(RMI)U54MH074404 · NIMH · SCRIPPS RESEARCH INSTITUTE, THE · PI ROSEN, HUGH · 2005 to 2007
$11.6M
Structure, Mechanism, and Engineering of Assembly Line Polyketide SynthasesR01GM087934 · NIGMS · STANFORD UNIVERSITY · PI KHOSLA, CHAITAN · 2009 to 2021
$4.9M
NIGMS NIH HHS R01 GM 087934NIGMS NIH HHS R01 GM087934NIMH NIH HHS 5U54MH074404NIMH NIH HHS U54 MH074404PHS HHS R01 AL 41014
6 · The paper itself

Abstract

Macrolide antibacterial agents inhibit parasite proliferation by targeting the apicoplast ribosome. Motivated by the long-term goal of identifying antiparasitic macrolides that lack antibacterial activity, we have systematically analyzed the structure-activity relationships among erythromycin analogues and have also investigated the mechanism of action of selected compounds. Two lead compounds, N-benzylazithromycin (11) and N-phenylpropylazithromycin (30), were identified with significantly higher antiparasitic activity and lower antibacterial activity than erythromycin or azithromycin. Molecular modeling based on the cocrystal structure of azithromycin bound to the bacterial ribosome suggested that a substituent at the N-9 position of desmethylazithromycin could improve selectivity because of species-specific interactions with the ribosomal L22 protein. Like other macrolides, these lead compounds display a strong "delayed death phenotype"; however, their early effects on T. gondii replication are more pronounced.

Indexed as

Anti-Bacterial AgentsAntiparasitic AgentsCells, CulturedHumansMacrolidesMagnetic Resonance SpectroscopyMicrobial Sensitivity TestsModels, MolecularSpectrometry, Mass, Electrospray IonizationStructure-Activity RelationshipToxoplasmaAnti-Bacterial AgentsAntiparasitic AgentsMacrolides

Identifiers

PMID21428405
PMCPMC3085955
OpenAlexW1978862189

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.