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Record W4387417611 · doi:10.5267/j.ccl.2023.8.003

Multicomponent approach to the synthesis and spectral characterization of some 3,5-pyrazolididione derivatives and evaluation as anti-inflammatory agents

2023· article· en· W4387417611 on OpenAlexvenueno aff
Yasser A. El‐Ossaily, Nuha M. M. Alanazi, Ibrahim O. Althobaiti, Hamud A. Altaleb, Nayef S. Al‐Muailkel, Mohamed Y. El‐Sayed, Modather F. Hussein, Ibrar Ahmed, Maha M. Alanazi, Ahmed Fawzy, Shaban A. A. Abdel‐Raheem, Mahmoud S. Tolba

Bibliographic record

VenueCurrent Chemistry Letters · 2023
Typearticle
Languageen
FieldChemistry
TopicSynthesis and biological activity
Canadian institutionsnot available
Fundersnot available
KeywordsChemistryDiethyl malonatePhenylhydrazinePyrazolonesYield (engineering)PyrazoloneImidazolePyrazoleMalononitrileCatalysisOrganic chemistry

Abstract

fetched live from OpenAlex

Pyrazolones are a class of heterocyclic compounds that contain a pyrazole ring fused to a ketone group. Recent scientific research has focused extensively on the potential anti-inflammatory properties of pyrazolone compounds due to their diverse pharmacological effects in alleviating inflammation and reducing fever. This motivated us to focus on the preparation of these derivatives in a simple and eco-friendly manner. A convenient new green methodology was modified for the preparation of 1-phenyl-3,5-pyrazolidinedione by the sonicated MCR of diethyl malonate, phenylhydrazine, and a catalytic amount imidazole as homogenous organic catalyst in water green solvent in a good yield. On the other hand, some of 4-arylidinepyrazolidinedione derivatives are prepared in the same manner via the treatment of a mixture of diethyl malonate, phenylhydrazine, aromatic aldehydes, and a catalytic amount of imidazole in an aqueous medium. Our target synthesized pyrazolidinediones were elucidated via elemental and several spectral analyses. Due to the importance of pyrazolidinediones in the field of treating inflammation and relieving pain, a number of prepared compounds were chosen to test their efficacy as anti-inflammatory agents using carrageenan-induced foot edema in rats and compare the results with indomethacin, the standard drug. We found that the majority of derivatives yield promising results spanning from good to wonderful, so derivatives (15k, 15b, 15h, 15a, and 15j) yield the best results while derivative (15i) yields an average result. As for the derivative (15f), it yields the lowest results compared to the standard drug. This is due to the difference in the structural composition of these derivatives, which increases the likelihood of their use as anti-inflammatory derivatives.

Fetched live from OpenAlex and de-inverted. Abstracts are not stored in this database: the inverted indexes are 8.6 GB of the frame’s 9.3 GB of text, and the host has 13 GB free.

How this classification was reachedexpand

Full frame machine prediction

Teacher imitation

Not calibrated prevalence, not ground truth. Human validation pending. The Gemma side is a direct model label for every work in the frame, read from the title-only record. The Codex side is a classifier learned from the 10,348 direct Codex labels and calibrated to design-weighted sample rates; fields without enough sample support carry no Codex call. Candidate is the union of the two sides; consensus is their intersection. These outputs are machine_predicted_unvalidated and are not human labels.

metaresearch head score (Codex)0.000
metaresearch head score (Gemma)0.000
Version: metacan-v3-hybrid-931329e0061cValidation status: machine_predicted_unvalidated
Candidate categoriesnone
Consensus categoriesnone
DomainCandidate signal: none · Consensus signal: none
Study designCandidate signal: Bench or experimental · Consensus signal: Bench or experimental
GenreCandidate signal: Empirical · Consensus signal: Empirical
Teacher disagreement score0.002
Threshold uncertainty score0.006

Distilled classifier scores by category (both heads)

CategoryCodexGemma
Metaresearch0.0000.000
Meta-epidemiology (narrow)0.0000.000
Meta-epidemiology (broad)0.0000.000
Bibliometrics0.0010.001
Science and technology studies0.0000.000
Scholarly communication0.0000.000
Open science0.0000.000
Research integrity0.0000.001
Insufficient payload (model declined to judge)0.0020.001

Machine scores (provisional)

The two teacher heads of the student model, read on this work. A score orders the frame for review; it never asserts a category, and the validation status ships verbatim with every row.

Baseline scores from an immature model (maturity gate not passed, 7 training rounds). Scores rank; they never assert a category.

Opus teacher head0.044
GPT teacher head0.272
Teacher spread0.227 · how far apart the two teachers sit on this one work
Validation statusscore_only:v0-immature-baseline · verbatim from the scoring run: score_only means the number may rank works, and no category label ships from it

Classification

machine, unvalidated

Machine predicted; a candidate call from one source (direct Gemma or distilled Codex), not a consensus.

The models applied no category: nothing in the taxonomy fit this work.
Study designBench or experimental
Domainnot available
GenreEmpirical

How this classification was reached, model by model and score by score, is at the end of the page under "How this classification was reached".

Quick stats

Citations14
Published2023
Admission routes1
Has abstractyes

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