Evaluation of the anti-inflammatory and anti-nociceptive activities of novel synthesized melatonin analogues

Elmegeed, Gamal A.; Baiuomy, Ayman R.; Abdel-Salam, Omar M.E.

doi:10.1016/j.ejmech.2007.01.027

Cited by 78 publications

(33 citation statements)

References 26 publications

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“…Melatonin is also involved in the regulation of other systems such as the pain system. In fact, the antinociceptive effect of melatonin has been demonstrated in animal models of acute pain (Li et al 2005;Ucar et al 2005;Elmegeed et al 2007), inflammatory pain (Arreola-Espino et al 2007), and neuropathic pain (Ulugol et al 2006). Preliminary studies in humans have shown melatonin effects on some pain syndromes, especially fibromyalgia (Citera et al 2000) and acute postoperative pain (Acil et al 2004;Caumo et al 2009).…”

Section: Introductionmentioning

confidence: 95%

Effect of exogenous melatonin administration on pain threshold in exercise trained rats under light-induced functional pinealectomy

Özkaya

Seyran

Hindistan

et al. 2014

Biological Rhythm Research

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Exercise-induced hypoalgesia (EIH) typically reported during and/or following exercise, but less is known the mechanisms responsible for EIH. Previous reports suggest that melatonin plays a role in pain modulation. In this study, we investigated the role of melatonin on pain threshold at rest, and following exercise in both sedentary and exercise trained rats under light-induced functional pinealectomy. Male wistar rats were assigned to one of four groups: sedentary control (C), sedentary pinealectomized (Px), exercise trained (T), and trained under pinealectomy (T-Px) groups. Exercise trained groups were subjected to eight weeks of motor-driven treadmill exercise. C and T groups exposed to normal light/dark cycle (12:12-h light/dark cycle) and Px and T-Px rats exposed to continuous light for eight weeks. Hot-plate test was repeated before and after melatonin injection and paw withdrawal latencies were recorded as pain threshold. Acute exercise resulted increased pain threshold in all groups. Animals in T group had significantly highest pain thresholds compared with other groups, and pinealectomy resulted decreased pain threshold in trained animals both at rest, and following exercise. Pain threshold in T-Px group was found to be increased after melatonin administration. Our findings support the hypothesis that melatonin plays a role on hypoalgesic response in exercise-trained rats.

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Section: Introductionmentioning

confidence: 95%

Effect of exogenous melatonin administration on pain threshold in exercise trained rats under light-induced functional pinealectomy

Özkaya

Seyran

Hindistan

et al. 2014

Biological Rhythm Research

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“…1). Elucidation of the proposed structures 8 and 9 was based on their correct elemental analyses and compatible IR, 1 H-NMR, 13 C-NMR, and mass spectral data (Experimental Section).…”

Section: Resultsmentioning

confidence: 99%

“…The heterocyclic antidepressants are the mainstay of antidepressant treatment and the development of new synthetic heterocyclic compounds as antidepressant, sedative, or analgesic agents has progressed considerably during the past decade [8][9][10]. In the scope of a research program aimed at the development of new alternatives to treat neurological disorders [11][12][13], in the present study, we describe the synthesis of new functionalized bi-heterocyclic or tri-heterocyclic compounds ( Fig. 1) attached to the essential pharmacophoric features of the TRP molecule.…”

Section: Introductionmentioning

confidence: 98%

Synthesis and Antidepressant Evaluation of Five Novel Heterocyclic Tryptophan‐Hybrid Derivatives

Elmegeed

Baiuomy

Abdelhalim

et al. 2010

Archiv der Pharmazie

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This study aimed at evaluating the reactivity of L-Tryptophan (TRP) 1 towards various chemical reagents to produce new bi- and tri-heterocyclic systems providing basic pharmacological activities. Indol-3-yl hydroxyoxazol-2-yl acetonitrile derivatives 5 and 6, indol-3-yl-hydroxyoxazol-2-yl-1,2,4-triazine derivatives 8 and 9, indol-3-yl-hydroxyoxazol-2-yl-aminopyrazole derivatives 11a, b, and indol-3-yl-hydroxyoxazol-2-yl-aminoisoxazole derivative 12 were synthesized via straightforward and efficient methods. The structures were characterized by spectral data (IR, (1)H-NMR, (13)C-NMR, and MS) and the purity was ascertained by microanalysis. Also, this work was extended to study the potential role of the novel synthesized TRP derivatives 5, 6, 9, 11a, and 12 as antidepressant and sedative agents in comparison with TRP. All compounds showed significant antidepressant activity in the forced-swimming test at two doses (50 or 100 mg/kg). Also, all tested compounds (at 50 or 100 mg/kg) produced a significant decrease in locomotor activity of mice during a 30 min observation period. The most potent antidepressant and sedative effect was produced by the tri-heterocyclic compounds 9 and 12, followed by 11a and TRP.

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“…Complex pyrroles are important syntons to macromolecular chemistry, environmental chemistry, medical chemistry, optics or nano-technologies [1][2][3][4][5].Asmonomers, pyrroles have demonstrated to possess antimicrobial [6], fungicide [7], antileukemic [8], analgesic [9] and anti-inflammatory [10] and anti-HIV-1 [11] activities.The title compound was synthesized within aproject of studying N-aryl substituted pyrrolesa sp otential anti-HIV-1 and/or anti-influenza drugs. In the title molecule, the angle between the mean planes of the pyrrole and phenyl rings is 57.82(7)°.The carboxylic group is also twisted around the C-C bond with an angle of 20.5(2)°between the mean planes of the carboxylic group and the phenyl ring.…”

Section: Discussionmentioning

confidence: 99%

Crystal structure of 2,5-dimethyl-1-(4-carboxyphenyl)pyrrole, C13H13NO2

Silva¹,

Silva²,

Urbano³

et al. 2008

Zeitschrift Für Kristallographie - New Crystal Structures

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C 13 H 13 NO 2 ,orthorhombic, Pbcn (no. 60), a =12.4741(2) Å, b =11.1481(2) Å, c =16. Source of materialTo asolutionofthe 4-aminobenzoic acid (1 mmol)and 2,5-hexadione (1.2 mmol) in THF (10 mL) at room temperature was added iodine (0.1 mmol). The mixture was stirred at this temperature with an N 2 positiveflow for aperiod of 2hours. Dichloromethane (20 mL) was then added to the mixture. The resulting mixture was washed successively with 5%N a 2 S 2 O 3solution (2 mL), saturated NaHCO3 solution (2 mL), and brine (2 mL). The organic layerwas then dried with sodium sulfate and concentrated. The product obtained was then purifiedbyflash chromatography with dichoromethane as novel phase and after completeevaporation of the solvent, 0.611 gof4-(2,5-dimethyl-pyrrol-1-yl)-benzoic acid were obtained. The compoundwas recrystallized from dichloromethane. Experimental detailsThe atomic coordinates of the carboxylic Hatom were freely refined and two alternative positions were allowed for this atom, either closer to O1 either closer to O2. The occupancy of each site refined to near 50 %.

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Evaluation of the anti-inflammatory and anti-nociceptive activities of novel synthesized melatonin analogues

Cited by 78 publications

References 26 publications

Effect of exogenous melatonin administration on pain threshold in exercise trained rats under light-induced functional pinealectomy

Effect of exogenous melatonin administration on pain threshold in exercise trained rats under light-induced functional pinealectomy

Synthesis and Antidepressant Evaluation of Five Novel Heterocyclic Tryptophan‐Hybrid Derivatives

Crystal structure of 2,5-dimethyl-1-(4-carboxyphenyl)pyrrole, C13H13NO2

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