Chemistry and Pharmacology of Acetanilide Derivatives: A Mini Review

Singh, Rajib Kumar; Kumar, Arvind; Mishra, Arun Kumar

doi:10.2174/1570178615666180808120658

Cited by 7 publications

(3 citation statements)

References 29 publications

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“…XIX в., когда два молодых врача Арнольд Чан и Пол Хеппа в борьбе с гельминтами по ошибке ввели пациенту вместо нафталина ацетанилид. Пациент почувствовал облегчение от боли и лихорадки, и с 1886 г. благодаря этому открытию препарат стал использоваться в медицинской практике под названием «антифебрин» [3]. Востребованность его была недолгой, т. к. ацетанилид обладал высокой токсичностью.…”

Section: парацетамол: от истории к современностиunclassified

Paracetamol and ibuprofen in the treatment of pain and fever in children: modern views on the choice of a drug

Zakharova,

Berezhnaya,

Pupykina

et al. 2023

Medicinskij sovet

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Paracetamol (acetaminophen) and ibuprofen are commonly used to relieve fever and pain in children. Their effects are similar, but differ in strength and mechanisms of action on the body. Acetaminophen, a para-aminophenol derivative, has antipyretic and analgesic properties. Despite the fact that paracetamol has been officially used as a drug for more than 75 years, its mechanism of biological action has not been sufficiently studied. In paediatric practice, paracetamol is more often used as an antipyretic, but in recent years, with the development of technology and emergence of new dosage forms on the market, it came into common use as an analgesic in many diseases, including oncological, rheumatological, etc. Ibuprofen is the most commonly used non-steroidal anti-inflammatory drug with pronounced analgesic and antipyretic properties. Ibuprofen, a non-selective inhibitor of cyclooxygenase-1 (COX-1) and cyclooxygenase-2 (COX-2), affects the hypothalamic thermoregulatory center via inhibition of prostaglandin synthesis. In the paediatric population, the most common indications for the use of ibuprofen are fever, sore throat, ear pain, headache and toothache, post-traumatic and musculoskeletal pain, and inflammatory joint diseases. Paracetamol and ibuprofen are safe for use in paediatric practice, if dosing rules are observed, and are approved for use by the World Health Organization, FDA and other expert organizations. In addition, the emergence of new presentation forms of these drugs is most important in paediatrics.

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Section: парацетамол: от истории к современностиunclassified

Paracetamol and ibuprofen in the treatment of pain and fever in children: modern views on the choice of a drug

Zakharova,

Berezhnaya,

Pupykina

et al. 2023

Medicinskij sovet

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“…This group is present, for example, on the structure of the analgesic and antipyretic drugs acetanilide (N-phenylacetamide) and paracetamol (N-acetyl-para-aminophenol). From this, other acetamide derivatives were introduced in the pharmaceutical field with varied activity [38,39]. A study by Kaplancikli et al [39] with acetamide derivatives demonstrated that new drugs having the acetamide group attached to benzothiazole and tetrazole rings contribute to reducing the nociceptive response.…”

Section: Isolation and Structure Elucidation Of The Degradation Productmentioning

confidence: 99%

Luliconazole: Stability-indicating LC method, structural elucidation of major degradation product by HRMS and in silico studies

Porto

Bajerski

Malesuik

et al. 2021

Rev. Colomb. Cienc. Quím. Farm.

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Aim: A new stability-indicating liquid chromatography method was developed and validated for the quantitative determination of luliconazole. Materials and methods: Preliminary forced degradation study demonstrated an additional peak of the degradation product at the same retention time to the drug, due to this, the method was developed optimizing the chromatographic conditions to provide sufficient peak resolution (R ≥ 2). The experimental design was evaluated to assess the robustness and the best chromatographic conditions to be used for the validation. Methodology: Luliconazole solutions were exposed to various stress conditions to evaluate the method indication stability, in which the degradation product (DP-1) formed was isolated, identified, and evaluated in silico to predict degradation pathway and toxicity. The procedure was validated by robustness, selectivity, linearity, precision, and accuracy. Liquid chromatography was performed in a Phenomenex® RP-18 column with a mixture of acetonitrile and 0.3% (v/v) triethylamine solution as a mobile phase in isocratic elution. Results and conclusions: The method demonstrated robustness, good recovery, precision, linear response over a range from 5.0 to 40.0 μg.mL-1, and to be stability indicating. The alkaline stress condition resulted in the formation of DP-1. hrms studies identified this product as an hydroxyacetamide derivative, and in silico studies did not show toxic potential.

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“…Besides, compounds bearing acetanilide structural moieties are widely used in pharmaceuticals (analgesic, anti-inflammatory, antipyretic, anticonvulsant, anticancer, antioxidative, antimalarial) and agrochemical industries. 6–9 Some representative examples include acetanilide, the well-known paracetamol, propanil and 2,2′-thiobis[ N -(4-chlorophenyl)acetamide] (Fig. 1).…”

Section: Introductionmentioning

confidence: 99%