Evidence map›Paper›PMID 28665338›Full record

ArticleMolecules (Basel, Switzerland)2017

Molecular Docking and Anticonvulsant Activity of Newly Synthesized Quinazoline Derivatives.

Hatem A Abuelizz, Rabab El Dib, Mohamed Marzouk, El-Hassane Anouar, Yousreya A Maklad, Hanan N Attia, Rashad Al-Salahi

Abstract read
In one paragraph

Article in Molecules (Basel, Switzerland), 2017. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 17 papers.

0numbers the graph read from it
0cells of the map it votes in
17citing 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

17 citing papers in PubMed.

  1. Article
  2. Article
  3. Article
  4. Review
  5. Review
  6. Molecules (Basel, Switzerland) · 2023
    Article
  7. Article
  8. Review
  9. Quinazolinones, the Winning Horse in Drug Discovery.Molecules (Basel, Switzerland) · 2023
    Review
  10. Novel 3-chloro-6-nitro-1Journal of enzyme inhibition and medicinal chemistry · 2022
    Article
  11. Article
  12. Two flavonoid-based compounds fromJournal of microbiology and biotechnology · 2020
    Article
  13. Article
  14. Article
  15. Article
  16. Article
  17. 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

7 authors.

Hatem A AbuelizzDepartment of Pharmaceutical Chemistry, College of Pharmacy, King Saud University, Riyadh 11451, Saudi Arabia. Habuelizz@ksu.edu.sa.
Rabab El DibDepartment of Pharmacognosy, College of Pharmacy, King Saud University, Riyadh 11495, Saudi Arabia. reldib@yahoo.com.
Mohamed MarzoukDepartment of Chemistry, College of Science and Humanities, Prince Sattam bin Abdulaziz University, P.O. Box 83, Alkharj 11942, Saudi Arabia. msmarzouk@yahoo.co.uk.
El-Hassane AnouarDepartment of Chemistry, College of Science and Humanities, Prince Sattam bin Abdulaziz University, P.O. Box 83, Alkharj 11942, Saudi Arabia. anouarelhassane@yahoo.fr.
Yousreya A MakladMedicinal and Pharmaceutical Chemistry Department (Pharmacology group), Pharmaceutical and Drug Industries Research Division, National Research Centre, Dokki, Giza 12622, Egypt. yousreya_maklad@yahoo.com.
Hanan N AttiaMedicinal and Pharmaceutical Chemistry Department (Pharmacology group), Pharmaceutical and Drug Industries Research Division, National Research Centre, Dokki, Giza 12622, Egypt. hanan_naeim@yahoo.com.
Rashad Al-SalahiDepartment of Pharmaceutical Chemistry, College of Pharmacy, King Saud University, Riyadh 11451, Saudi Arabia. ralsalahi@ksu.edu.sa.

Funding

No grant is acknowledged in the PubMed record.

6 · The paper itself

Abstract

A new series of quinazoline-4(3H)-ones are evaluated for anticonvulsant activity. After intraperitoneal (ip) injection to albino mice at a dose of 100 mg/kg body weight, synthesized quinazolin-4(3H)-ones (1-24) were examined in the maximal electroshock (MES) induced seizures and subcutaneous pentylenetetrazole (scPTZ) induced seizure models in mice. The Rotarod method was applied to determine the neurotoxicity. Most of the compounds displayed anticonvulsant activity in the scPTZ screen at a dose range of 0.204-0.376 mmol/mL. Out of twenty-four, compounds 8, 13 and 19 proved to be the most active with a remarkable protection (100%) against PTZ induced convulsions and four times more potent activity than ethosuximide. The structure-activity relationship concluded valuable pharmacophoric information, which was confirmed by the molecular docking studies using the target enzyme human carbon anhydrase II (HCA II). The studied quinazoline analogues suggested that the butyl substitution at position 3 has a significant effect on preventing the spread of seizure discharge and on raising the seizure threshold. However, benzyl substitution at position 3 has shown a strong anticonvulsant activity but with less seizure prevention compared to the butyl substitution.

Indexed as

Molecular Docking SimulationMolecular Dynamics SimulationAnimalsAnticonvulsantsDisease Models, AnimalHumansMaleMiceQuinazolinesSeizuresStructure-Activity RelationshipAnticonvulsantsQuinazolinesanticonvulsantethosuximidemolecular dockingphenobarbitalquinazolines

Identifiers

PMID28665338
PMCPMC6152033

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.