Evidence map›Paper›PMID 35860526›Full record

ArticleDrug design, development and therapy2022

Design, Synthesis, and Anti-Inflammatory Activity of Some Coumarin Schiff Base Derivatives: In silico and in vitro Study.

Shokhan J Hamid, Twana Salih

Abstract read
In one paragraph

Article in Drug design, development and therapy, 2022. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 9 papers.

0numbers the graph read from it
0cells of the map it votes in
9citing 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

9 citing papers in PubMed.

  1. Article
  2. Article
  3. Article
  4. Article
  5. Coumarin: A natural solution for alleviating inflammatory disorders.Current research in pharmacology and drug discovery · 2024
    Review
  6. Review
  7. Article
  8. Article
  9. 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

2 authors.

Shokhan J HamidDepartment of Pharmacognosy and Pharmaceutical Chemistry, College of Pharmacy, University of Sulaimani, Sulaymaniyah, Iraq.ORCID 0000-0002-6831-9814
Twana SalihDepartment of Pharmacognosy and Pharmaceutical Chemistry, College of Pharmacy, University of Sulaimani, Sulaymaniyah, Iraq.ORCID 0000-0002-7684-8601

Funding

No grant is acknowledged in the PubMed record.

6 · The paper itself

Abstract

Introduction: Inflammation is a fundamental response of the immune system during tissue damage or pathogen infection to protect and maintain tissue homeostasis. However, inflammation may lead to life-threatening conditions. The most common treatment of inflammation is non-steroidal anti-inflammatory drugs (NSAIDs). Nowadays, the development of safer new NSAIDs is critical as most of the existing NSAIDs have serious adverse effects, such as gastrointestinal (GI) toxicity and cardiotoxicity. In the present study, four compounds as Schiff base derivatives of 7-hydroxy-4-formyl coumarin and 7-methoxy-4-formyl coumarin were designed and synthesized aiming to develop a lead compound that exhibits anti-inflammatory activity and circumvents the side effects of NSAIDs, especially GI toxicity. Materials and Methods: Lipinski's rule of five was applied for each designed molecule to evaluate the drug-likeness properties. Molecular docking studies were performed using the ligands and the cyclooxygenase-2 (COX-2) protein to select the best-scored molecule using AutoDock 4.2.6. The molecules were then synthesized and characterized. An in vitro anti-inflammatory assay of the compounds against the COX-2 receptor was realized through a protein denaturation assay. Results and Discussion: All four synthesized ligands passed Lipinski's rule of five and exhibited higher binding free energy compared to the positive standard control (ibuprofen), and the Conclusion: The present study suggested that compound 7 may be a lead molecule because this ligand not only exhibited the best computational and experimental results but also exhibited the strongest correlation between the concentration and percentage of protein denaturation (R = 0.986 and R

Indexed as

Cyclooxygenase 2 InhibitorsSchiff BasesAnti-Inflammatory AgentsAnti-Inflammatory Agents, Non-SteroidalCoumarinsCyclooxygenase 2HumansIbuprofenInflammationLigandsMolecular Docking SimulationAnti-Inflammatory AgentsAnti-Inflammatory Agents, Non-SteroidalCoumarinsCyclooxygenase 2Cyclooxygenase 2 InhibitorsIbuprofenLigandsSchiff Basesbinding free energycoumarincyclooxygenaseibuprofenlead compoundnon-steroidal anti-inflammatory drugsSchiff base derivatives

Identifiers

PMID35860526
PMCPMC9293384

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Registered trials

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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.