Events8th International Electronic Conference on Medicinal Chemistry
Published
with-doi10.3390/ECMC2022-13288 (registering DOI)
This submission belongs to the session S4. Small molecules as drug candidates of the event 8th International Electronic Conference on Medicinal Chemistry
Published date
01 Nov, 2022
Academic Editor
author-avatarAlfredo Berzal-Herranz
Citation
Vladimir Dobričić, Nikola Nedeljković, Marina Mijajlović, Jovana Bradić, Marijana Anđić, Aleksandar Kočović, Nevena Jeremić, Jovana Jeremić, Vladimir Jakovljević, Zorica Vujić, Miloš Nikolić, Anti-inflammatory activity of selected thiourea derivatives of naproxen on carrageenan induced paw edema in Wistar albino rats, in Proceedings of 8th International Electronic Conference on Medicinal Chemistry, 1 November–30 November 2022, MDPI: Basel, Switzerland, doi: 10.3390/ECMC2022-13288
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Anti-inflammatory activity of selected thiourea derivatives of naproxen on carrageenan induced paw edema in Wistar albino rats

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1. University of Kragujevac, Serbia, Faculty of Medical Sciences, Department of Pharmacy
2. Department of Pharmaceutical Chemistry, University of Belgrade - Faculty of Pharmacy, Belgrade, Serbia, Serbia
3. University of Kragujevac, Serbia, Faculty of Medical Sciences, Department of Physiology
4. Department of Human Pathology, First Moscow State Medical University IM Sechenov, Moscow, Russia
5. Department of Pharmaceutical Chemistry, University of Belgrade – Faculty of Pharmacy, Belgrade, Serbia
Abstract

In previous studies, the thiourea derivatives of non-steroidal anti-inflammatory drugs demonstrated significant anti-inflammatory activity. In this pilot study, three thiourea derivatives of naproxen were selected from the initial group of synthesized compounds for evaluation of anti-inflammatory activity using carrageenan induced paw edema model of acute inflammation. Analyzed compounds contained ethyl ester of L-phenylalanine, p-methoxyaniline and p-ethoxyaniline in the side chains. Wistar albino male rats were divided into 9 test groups and 4 control groups. Test groups were treated with different oral doses of selected thiourea derivative of naproxen: 2.5 mg/kg, 5 mg/kg and 10 mg/kg body weight. Three control groups were treated with 2.5 mg/kg, 5 mg/kg and 10 mg/kg body weight of naproxen and one control group was treated with solvent 1% DMSO. The thickness of the left paw tissue of each rat was measured using a Digital Vernier caliper at the following time intervals: immediately before inducing inflammation and 1, 2, 3 and 4 hours after inflammation. All tested compounds in every tested dose in the fourth hour after carrageenan administration showed a statistically significant (p < 0.05) inhibitory effect on the increase of rat paw edema compared to control, except for L-phenylalanine ethyl ester derivative in dose of 5 mg/kg and p-ethoxyaniline derivative in dose of 2.5 mg/kg. The highest percentage of inhibition was exhibited by L-phenylalanine ethyl ester and p-methoxyaniline derivatives (10 mg/kg) in the last hour (81.81%). According to obtained results, L-phenylalanine ethyl ester derivative stood out for its dose- and time-dependent anti-inflammatory effect.

Keywords
thiourea
naproxen
carrageenan
paw edema
anti-inflammatory activity
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