ChemInform Abstract: A Brief Review on Recent Synthesis of 2‐Azetidinone Derivatives

Salunkhe, Dhairyashil S; Piste, Pravina B.

doi:10.1002/chin.201515340

Cited by 5 publications

(5 citation statements)

References 9 publications

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“…As a result of those studies and being endowed with a unique structure, azetidin-2-ones proved to be potent antibacterials (β-lactam antibiotics), including penicillins, cephalosporins, carbapenems, monobactams, clavulanic acid, sulbactam, and tazobactam [4]. Recently, the azetidin-2-one scaffold has provided compounds with a wide spectrum of activities, such as cholesterol absorption inhibitory (Ezetimibe), anticancer, antitubercular, antidiabetic, anti-inflammatory, analgesic, thrombin inhibition, antiparkinsonian, vasopressin antagonist, anticonvulsant, enzyme inhibitors [5,6].…”

Section: Introductionmentioning

confidence: 99%

Biological Evaluation of Azetidine-2-One Derivatives of Ferulic Acid as Promising Anti-Inflammatory Agents

et al. 2020

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The purpose of this study was to evaluate the in vivo biological potential of new azetidine-2-one derivatives of ferulic acid (6a–f). First, the in vivo acute toxicity of azetidine-2-one derivatives of ferulic acid on Swiss white mice was investigated and, based on the obtained results, it can be stated that the studied derivatives belong to compounds with moderate toxicity. The in vivo anti-inflammatory potential of these derivatives was determined in a model of acute inflammation induced by carrageenan in rats and in a chronic inflammation model induced in rats using the granuloma test. In the acute inflammation model, all the studied compounds had a maximum anti-inflammatory effect 24 h after administration, which suggests that these compounds may be classified, from a pharmacokinetic point of view, in the category of long-acting compounds. The most active compound in the series was found to be compound 6b. In the case of the chronic inflammation model, it was observed that the studied compounds (6a–f) reduced the formation of granulation tissue compared to the control group, having an intense effect of inhibiting the proliferative component. The most important inhibitory effect of inhibiting the proliferative component was recorded for compound 6b. Additionally, the investigation of liver function was performed by determining the serum levels of liver enzymes aspartate transaminase (AST), alanine aminotransferase (ALT), lactate dehydrogenase (LDH) and bilirubin (total and direct). The results showed that, in the series of azetidin-2-one derivatives, the liver enzymes concentration values were close to those recorded for the reference anti-inflammatories (diclofenac sodium and indomethacin) and slightly higher compared to the values for the healthy control group. At the end of the experiment, the animals were euthanized and fragments of liver, lung, and kidney tissue were taken from all groups in the study. These were processed for histopathological examination, and we noticed no major changes in the groups treated with the azetidine 2-one derivatives of ferulic acid compared to the healthy groups.

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Section: Introductionmentioning

confidence: 99%

Biological Evaluation of Azetidine-2-One Derivatives of Ferulic Acid as Promising Anti-Inflammatory Agents

et al. 2020

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“…Finally, we are interested in heterocyclic compounds as we found that four-membered ring azitidinones derivatives are a key component group of heterocyclic compounds that have a wide range of biological activities it acts as anticancer, (Salunkhe and Piste, 2014) antimicrobial, (Bagherwal et al, 2011) antibacterial, antifungal, (Patel et al, 2011) and anti-inflammatory, (Rajasekaran et al, 2010) These compounds were prepared through the reaction of Schiff bases with chloroacetylchloride.…”

Section: Introductionmentioning

confidence: 99%

Synthesis of some New Derivatives of Triazole using Ortho-Carboxybenzaldehyde as a Synthone

Khder¹,

noori²

2022

RJS

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In this work, the 1,2,4-triazole ring was prepared by introducing the starting material ortho-carboxybenzaldehyde (1) in the usual esterification reaction, in ethanol as a solvent and in the presence of concentrated sulfuric acid to give ethyl-2formylbenzoate (2), then introducing the resulting ester in a condensation reaction with thiosemberazide in the presence of ethanol as a solvent to afforded 2-(2-formylbenzoyl)hydrazine-1-carbothioamide (3), which on cyclisation using a solution of sodium hydroxide to obtain the 1,2,4-triazole compound (4), which on treatment with different primary aromatic amines to obtain Schiff bases (5a-e) the prepared Schiff bases were introduced into a reaction with chloroacetyl chloride in the presence of triethylamine as an auxiliary base for the reaction to prepare the tetracyclic azitidinone compounds (beta-lactams) (6a-e) along with the triazole ring in the same compound. Finally, these prepared compounds were characterized by physical and spectroscopic measurements such as melting point, thin layer chromatography (m.p., TLC) infrared spectroscopic measurements FT-IR, and nuclear magnetic resonance spectra of some compounds 1 H-NMR.

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“…four membered ring azitidinones derivatives are an important group of heterocyclic compounds that have a wide range of biological activities it act as anticancer [3], antimicrobial [4], anti-bacterial, antifungal [5] and anti-inflammatory [6]. These compound were prepared through the reaction of Schiff bases with chloroacetylchloride.…”

Section: Introductionmentioning

confidence: 99%

Synthesis Of Some Heterocyclic Compounds Derived From Ortho-Carboxybenzaldehyde

Khder

Al-Jawady

2021

Egypt. J. Chem.

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In this work different heterocyclic compounds derivatives were synthesized using ortho-Carboxybenzaldehyde as a starting material which reacted with different aromatic amines to produce Schiff bases. These Schiff bases introduced in three types of reactions using different reagents (Chloroacetylchloride, Thio acetic acid, Malic anhydride and Phthalic anhydride) to give the target heterocyclic compounds four, five and seven heterocyclic compounds derivatives. The structure of these compounds identified by FT-IR and some of them by 1 H-NMR spectra

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ChemInform Abstract: A Brief Review on Recent Synthesis of 2‐Azetidinone Derivatives

Abstract: Review: 58 refs.

Cited by 5 publications

References 9 publications

Biological Evaluation of Azetidine-2-One Derivatives of Ferulic Acid as Promising Anti-Inflammatory Agents

Biological Evaluation of Azetidine-2-One Derivatives of Ferulic Acid as Promising Anti-Inflammatory Agents

Synthesis of some New Derivatives of Triazole using Ortho-Carboxybenzaldehyde as a Synthone

Synthesis Of Some Heterocyclic Compounds Derived From Ortho-Carboxybenzaldehyde

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