Synthesis and Pharmacological Evaluation of New Chemical Entities Based on Paracetamol and Their Ibuprofen Conjugates as Novel and Superior Analgesic and Anti-Inflammatory Candidates

Ahmadi, Abbas; Khalili, Mohsen; Ahmadian, Sepideh; Shahghobadi, Nadia; Nahri-Niknafs, Babak

doi:10.1007/s11094-014-1059-x

Cited by 13 publications

(2 citation statements)

References 20 publications

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“…It was noted that modifying the carboxyl group could lead to compounds that become more selective for COX-2 isoform. Some pharmacophores such as two aromatic rings seem to be also responsible for COX-2 selectivity by tting in the enzyme structure [20]. Starting from ibuprofen,new thiazolidin-4-one derivatives have been synthesized by our research group [7], as candidates to alleviate the pain or in ammation associated with various pathological conditions.…”

Section: Discussionmentioning

confidence: 99%

New ibuprofen derivatives with thiazolidin-4-one scaffold with improved pharmaco-toxicological profile

Vasincu

Apotrosoaei

Constantin

et al. 2020

Preprint

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Background Aryl-propionic acid derivatives with ibuprofen as representative drug are very important for therapy, being recommended especially for anti-inflammatory and analgesic effects. On other hand 1,3-thiazolidine-4-one scaffold is an important heterocycle, which is associated with different biological effects such as anti-inflammatory and analgesic, antioxidant, antiviral, antiproliferative, antimicrobial etc. The present study aimed to evaluated the toxicity degree and the anti-inflammatory and analgesic effects of new 1,3-thiazolidine-4-one derivatives of ibuprofen. Methods For evaluation the toxicity degree, cell viability assay using MTT method and acute toxicity assay on rats were applied. The carrageenan-induced paw-edema in rat was used for evaluation of the anti-inflammatory effect while for analgesic effect the tail-flick test, as thermal nociception in rats and the writhing assay, as visceral pain in mice, were used. Results The toxicological screening, in terms of cytotoxicity and toxicity degree on mice, revealed that the ibuprofen derivatives (4a-n) are non-cytotoxic at 2 µg/ml. In addition, ibuprofen derivatives reduced carrageenan-induced paw edema in rats, for most of them the maximum effect was recorded at 4 h after administration which means they have medium action latency, similar to that of ibuprofen. Moreover, for compound 4d the effect was higher than that of ibuprofen, even after 24 h of administration. The analgesic effect evaluation highlighted that 4 h showed increased pain inhibition in reference to ibuprofen in thermal (tail-flick assay) and visceral (writhing assay) nociception models. Conclusions The study revealed for ibuprofen derivatives, noted as 4 m, 4 k, 4e, 4d, a good anti-inflammatory and analgesic effect and also a safer profile compared with ibuprofen. These findings could suggest the promising potential use of them in the treatment of inflammatory pain conditions.

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Section: Discussionmentioning

confidence: 99%

New ibuprofen derivatives with thiazolidin-4-one scaffold with improved pharmaco-toxicological profile

Vasincu

Apotrosoaei

Constantin

et al. 2020

Preprint

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“…20 It was observed that the carboxyl group is responsible for the side-effects associated with NSAIDs in general and ibuprofen in particular including gastric ulceration and hepatic and renal complications. 21 Thus attachment of other moieties to the carboxyl group may have prolic effect on the overall pharmacological prole of ibuprofen. 22 In the current study, the salicylaldehyde was attached as imine moiety with the carboxylic group of ibuprofen (NS4).…”

Section: Gastric Protective Effectsmentioning

confidence: 99%

Bio-oriented synthesis of ibuprofen derivatives for enhancement efficacy in post-operative and chronic inflammatory pain models

et al. 2023

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Synthesis of New Acetaminophen Analogs and Their Ibuprofen Conjugates as Novel Analgesic Drugs

et al. 2016

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Synthesis and Pharmacological Evaluation of New Chemical Entities Based on Paracetamol and Their Ibuprofen Conjugates as Novel and Superior Analgesic and Anti-Inflammatory Candidates

Cited by 13 publications

References 20 publications

New ibuprofen derivatives with thiazolidin-4-one scaffold with improved pharmaco-toxicological profile

New ibuprofen derivatives with thiazolidin-4-one scaffold with improved pharmaco-toxicological profile

Bio-oriented synthesis of ibuprofen derivatives for enhancement efficacy in post-operative and chronic inflammatory pain models

Synthesis of New Acetaminophen Analogs and Their Ibuprofen Conjugates as Novel Analgesic Drugs

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