Evidence map›Paper›PMID 30145051›Full record

ArticleBioorganic & medicinal chemistry2018

An antimycobacterial pleuromutilin analogue effective against dormant bacilli.

Maddie R Lemieux, Shajila Siricilla, Katsuhiko Mitachi, Shakiba Eslamimehr, Yuehong Wang, Dong Yang, Jeffrey D Pressly, Ying Kong, Frank Park, Scott G Franzblau and 1 more

Abstract read
In one paragraph

Article in Bioorganic & medicinal chemistry, 2018. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 10 papers.

0numbers the graph read from it
0cells of the map it votes in
10citing papers in PubMed
1.7field-weighted citation impact, top 17% 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

10 citing papers in PubMed, 14 citations in OpenAlex.

  1. ComprehensiveFrontiers in veterinary science · 2025
    Article
  2. Article
  3. Article
  4. Article
  5. Article
  6. "Upcycling" known molecules and targets for drug-resistant TB.Frontiers in cellular and infection microbiology · 2022
    Article
  7. Targeting Non-ReplicatingInternational journal of molecular sciences · 2021
    Review
  8. Article
  9. Article
  10. 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

11 authors at 2 institutions in 1 country.

Maddie R LemieuxDepartment of Pharmaceutical Sciences, College of Pharmacy, University of Tennessee Health Science Center, 881 Madison Avenue, Memphis, TN 38163-0001, United States.
Shajila SiricillaDepartment of Pharmaceutical Sciences, College of Pharmacy, University of Tennessee Health Science Center, 881 Madison Avenue, Memphis, TN 38163-0001, United States.
Katsuhiko MitachiDepartment of Pharmaceutical Sciences, College of Pharmacy, University of Tennessee Health Science Center, 881 Madison Avenue, Memphis, TN 38163-0001, United States.
Shakiba EslamimehrDepartment of Pharmaceutical Sciences, College of Pharmacy, University of Tennessee Health Science Center, 881 Madison Avenue, Memphis, TN 38163-0001, United States.
Yuehong WangInstitute for Tuberculosis Research, College of Pharmacy, University of Illinois at Chicago, 833 S. Wood Street, Chicago, IL 60612, United States.
Dong YangDepartment of Microbiology, Immunology & Biochemistry, University of Tennessee Health Science Center, 858 Madison Avenue, Memphis, TN 38163-0001, United States.
Jeffrey D PresslyDepartment of Pharmaceutical Sciences, College of Pharmacy, University of Tennessee Health Science Center, 881 Madison Avenue, Memphis, TN 38163-0001, United States.
Ying KongDepartment of Microbiology, Immunology & Biochemistry, University of Tennessee Health Science Center, 858 Madison Avenue, Memphis, TN 38163-0001, United States.
Frank ParkDepartment of Pharmaceutical Sciences, College of Pharmacy, University of Tennessee Health Science Center, 881 Madison Avenue, Memphis, TN 38163-0001, United States.
Scott G FranzblauInstitute for Tuberculosis Research, College of Pharmacy, University of Illinois at Chicago, 833 S. Wood Street, Chicago, IL 60612, United States.
Michio KurosuDepartment of Pharmaceutical Sciences, College of Pharmacy, University of Tennessee Health Science Center, 881 Madison Avenue, Memphis, TN 38163-0001, United States. Electronic address: mkurosu@uthsc.edu.
University of Tennessee Health Science Center · USUniversity of Illinois Chicago · US

Funding

Mechanistic details of key integral-membrane enzymes for antimicrobial discoveryR01GM114611 · NIGMS · CALIFORNIA INSTITUTE OF TECHNOLOGY · PI William M. Clemons, Michio Kurosu · 2016 to 2026
$4.2M
Targeting MraY: Synthesis and Validation of MraY InhibitorsR01AI084411 · NIAID · UNIVERSITY OF TENNESSEE HEALTH SCI CTR · PI KUROSU, MICHIO · 2010 to 2013
$1.5M
Expansion of spectrum of activity of pleuromutilin for MDR Gram-negative bacteriaR21AI119796 · NIAID · UNIVERSITY OF TENNESSEE HEALTH SCI CTR · PI KUROSU, MICHIO · 2015 to 2016
$431k
NIAID NIH HHS R01 AI084411NIAID NIH HHS R21 AI119796NIGMS NIH HHS R01 GM114611
6 · The paper itself

Abstract

Pleuromutilin is a promising pharmacophore to design new antibacterial agents for Gram-positive bacteria. However, there are limited studies on the development of pleuromutilin analogues that inhibit growth of Mycobacterium tuberculosis (Mtb). In screening of our library of pleuromutilin derivatives, UT-800 (1) was identified to kill replicating- and non-replicating Mtb with the MIC values of 0.83 and 1.20 μg/mL, respectively. UT-800 also kills intracellular Mtb faster than rifampicin at 2× MIC concentrations. Pharmacokinetic studies indicate that 1 has an oral bioavailability with an average F-value of 27.6%. Pleuromutilin may have the potential to be developed into an orally administered anti-TB drug.

Indexed as

Administration, OralAnimalsAntitubercular AgentsArea Under CurveBiological AvailabilityCaco-2 CellsDiterpenesFemaleHalf-LifeHumansInhibitory Concentration 50MiceMice, Inbred BALB CMicrobial Sensitivity TestsMycobacterium tuberculosisPleuromutilinsAntitubercular AgentsDiterpenesPleuromutilinsPolycyclic CompoundsAntimycobacterial activityDormant tuberculosisIntracellular Mycobacterium tuberculosisPharmacokineticsPleuromutilin

Identifiers

PMID30145051
PMCPMC6154393
OpenAlexW2887471527

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.