Evidence map›Paper›PMID 29126738›Full record

ArticleEuropean journal of medicinal chemistry2018

Biphenylthiazole antibiotics with an oxadiazole linker: An approach to improve physicochemical properties and oral bioavailability.

Mohamed Hagras, Youssef A Hegazy, Amr H Elkabbany, Haroon Mohammad, Adel Ghiaty, Tamer M Abdelghany, Mohamed N Seleem, Abdelrahman S Mayhoub

Abstract read
In one paragraph

Article in European 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 10 papers.

0numbers the graph read from it
0cells of the map it votes in
10citing 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

10 citing papers in PubMed.

  1. Article
  2. Article
  3. Article
  4. Article
  5. Review
  6. Antimicrobial Activity of 1,3,4-Oxadiazole Derivatives.International journal of molecular sciences · 2021
    Review
  7. Article
  8. Review
  9. RSC advances · 2019
    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

8 authors.

Mohamed HagrasDepartment of Pharmaceutical Organic Chemistry, College of Pharmacy, Al-Azhar University, Cairo 11884, Egypt.
Youssef A HegazyDepartment of Comparative Pathobiology, Purdue University, College of Veterinary Medicine, West Lafayette, IN, USA.
Amr H ElkabbanyDepartment of Pharmaceutical Organic Chemistry, College of Pharmacy, Al-Azhar University, Cairo 11884, Egypt.
Haroon MohammadDepartment of Comparative Pathobiology, Purdue University, College of Veterinary Medicine, West Lafayette, IN, USA.
Adel GhiatyDepartment of Pharmaceutical Organic Chemistry, College of Pharmacy, Al-Azhar University, Cairo 11884, Egypt.
Tamer M AbdelghanyDepartment of Pharmacology, College of Pharmacy, Al-Azhar University, Cairo 11884, Egypt.
Mohamed N SeleemDepartment of Comparative Pathobiology, Purdue University, College of Veterinary Medicine, West Lafayette, IN, USA; Purdue Institute for Inflammation, Immunology, and Infectious Diseases, West Lafayette, IN, USA.
Abdelrahman S MayhoubDepartment of Pharmaceutical Organic Chemistry, College of Pharmacy, Al-Azhar University, Cairo 11884, Egypt; Biomedical Sciences, University of Science and Technology, Zewail City of Science and Technology, Giza, Egypt. Electronic address: amayhoub@azhar.edu.eg.

Funding

Repurposing auranofin and ebselen for treatment of multidrug resistant pathogensR01AI130186 · NIAID · VIRGINIA POLYTECHNIC INST AND ST UNIV · PI SELEEM, MOHAMED · 2017 to 2021
$2.3M
NIAID NIH HHS R01 AI130186
6 · The paper itself

Abstract

A new series of oxadiazolylbiphenylthiazoles was prepared with the objective of improving the limited solubility of first-generation derivatives while maintaining antibacterial activity against drug-resistant Staphylococcus aureus. Studying the structure-activity relationship at the cationic part provided the piperazine-1-carboximidamide derivative 27 with a MIC (MRSA) value of 1.1 μg/mL, bactericidal mode of action, and a 50-fold improvement in aqueous solubility. Additionally, 27 exhibited a wider safety margin against mammalian cells, and most importantly, a significant improvement in oral bioavailability.

Indexed as

Chemical PhenomenaAdministration, OralAnimalsAnti-Bacterial AgentsBiological AvailabilityCell LineCricetinaeHumansMaleMethicillin-Resistant Staphylococcus aureusMicrobial Sensitivity TestsOxadiazolesRatsSolubilityStructure-Activity RelationshipThiazolesAnti-Bacterial AgentsOxadiazolesThiazolesAntibiotic drug resistanceCaenorhabditis elegansMethicillin-resistant Staphylococcus aureusMRSAPharmacokinetics

Identifiers

PMID29126738
PMCPMC5736435

What OpenQuestion holds

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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.