scholarly journals Synthesis, Characterization and Preliminary Anti-inflammatory Evaluation of New Etodolac Derivatives

2019 ◽  
Vol 28 (1) ◽  
pp. 106-112
Author(s):  
Omeed M. Hassan ◽  
Susan W. Sarsam
Keyword(s):  
Ir Spectroscopy ◽  
Egg White ◽  
Inflammatory Activity ◽  
Paw Edema ◽  
Ft Ir ◽  
Anti Inflammatory ◽  
Multistep Reaction ◽  
Derivatives Of ◽  
Ft Ir Spectroscopy ◽  
Inflammatory Effect

Three new hydrazone derivatives of Etodolac were synthesized and evaluated for their anti-inflammatory activity by using egg white induced paw edema method. All the synthesized target compounds were characterized by CHN- microanalysis, FT-IR spectroscopy, and 1HNMR analysis. The synthesis of the target (P1-P3) compounds was accomplished following multistep reaction procedures. The synthesized target compounds were found to be active in reducing paw edema thickness and their anti-inflammatory effect was comparable to that of the standard (Etodolac).

scholarly journals Synthesis, Characterization and Preliminary Anti-inflammatory Evaluation of New Fenoprofen Hydrazone Derivatives

2020 ◽  
Vol 29 (2) ◽  
pp. 239-244
Author(s):  
Hayder M. Abdulhamza ◽  
Muthanna S. Farhan
Keyword(s):  
Ir Spectroscopy ◽  
Egg White ◽  
Inflammatory Activity ◽  
Paw Edema ◽  
Ft Ir ◽  
Anti Inflammatory ◽  
Multistep Reaction ◽  
Derivatives Of ◽  
Ft Ir Spectroscopy ◽  
Inflammatory Effect

New hydrazone derivatives of Fenoprofen were synthesized and evaluated for their anti-inflammatory activity by means of egg white induced paw edema method. All the synthesized target compounds were characterized by FT-IR spectroscopy, 1HNMR analysis and by measure of their physical properties. The synthesis of the target compounds(H1-H4) was accomplished by multistep reaction procedures. The synthesized target compounds were show activity in reducing paw edema thickness and their anti-inflammatory effect was comparable to that of the standard (Fenoprofen) except for compound H3 which show anti-inflammatory activity higher than Fenoprofen.

scholarly journals Synthesis and Characterization of New Etodolac Derivatives with Possible Anti-Inflammatory Activity

2019 ◽  
Vol 28 (1) ◽  
pp. 107-113
Author(s):  
Omeed Muhsin Hassan ◽  
Susan Sarsam
Keyword(s):  
Ir Spectroscopy ◽  
Egg White ◽  
Inflammatory Activity ◽  
Synthesis And Characterization ◽  
Paw Edema ◽  
Ft Ir ◽  
Anti Inflammatory ◽  
Ft Ir Spectroscopy ◽  
Inflammatory Effect

A series of Etodolac hydrazone derivatives were synthesized and evaluated for their anti-inflammatory activity by using egg white induced paw edema method. All the synthesized target compounds were characterized by CHN- microanalysis, FT-IR spectroscopy and 1HNMR analysis. The synthesized target compounds (P1-P3) were found to be active in reducing paw edema thickness and their anti-inflammatory effect was comparable to that of the standard (Etodolac). Keywords: Etodolac hydrazone derivatives, anti-inflammatory, paw edemamethod.

scholarly journals SYNTHESIS AND PRELIMINARY PHARMACOLOGICAL EVALUATION OF NEW NAPROXEN ANALOGUES HAVING 1, 2, 4-TRIAZOLE-3-THIOL

2017 ◽  
Vol 9 (7) ◽  
pp. 66
Author(s):  
Monther F. Mahdi ◽  
Noor H. Naser ◽  
Nethal H. Hammud
Keyword(s):  
Aromatic Aldehydes ◽  
Heterocyclic Ring ◽  
Inflammatory Activity ◽  
Control Group ◽  
Paw Edema ◽  
Dose Equivalent ◽  
Edema Model ◽  
Anti Inflammatory ◽  
Derivatives Of

Objective: The objective of this search was to synthesize a new naproxen analogues having a 1,2,4-triazole-3-thiol heterocyclic ring, and preliminary pharmacological assessment of the anti-inflammatory activity of the synthesized compounds. Methods: The synthesis of naproxen analogues that having 1,2,4-triazole-3-thiol heterocyclic ring occur through esterification of naproxen, and then its reaction with hydrazine hydrate, and carbon disulfide, finally different aromatic aldehydes reacted with triazole derivatives of naproxen containing amino group to produce schiff bases.Results: In vivo acute anti-inflammatory activity of the synthesize compounds (Va-Vd) was evaluated in rats using egg-white induced edema model of inflammation in a dose equivalent to (50 mg/kg) of naproxen. All tested compounds were produced a significant reduction in paw edema with respect to the effect of propylene glycol 50% v/v (control group). Compound Vd produced superior anti-inflammatory activity compared to naproxen.Conclusion: The results obtained in this work give evidence about the valid synthesis of 1,2,4 triazole-3-thiol derivatives of naproxen, which reacted with different aldehydes to yield several schiff bases. The incorporation of benzaldehyde possess para-electron donating group (para-hydroxyl benzaldehyde) will increase the anti-inflammatory activity of naproxen.

scholarly journals Synthesis, Characterization and Acute Anti-inflammatory Evaluation of New Mefenamic Acid Derivatives Having 4-Thiazolidinone Nucleus

2019 ◽  
Vol 28 (1) ◽  
pp. 138-146
Author(s):  
Mustafa H. Ali Alsafi ◽  
Muthanna S. Farhan
Keyword(s):  
Side Effects ◽  
Mefenamic Acid ◽  
Paw Edema ◽  
Compound I ◽  
Reference Drug ◽  
Cox 2 ◽  
Anti Inflammatory ◽  
Derivatives Of ◽  
Cox 1 ◽  
Inflammatory Effect

Mefenamic acid (MA) is one of the non-steroidal anti-inflammatory drugs, it is widely used probably due to having both anti-inflammatory and analgesic activity, the main side effects of mefenamic acid include gastrointestinal tract (GIT) disturbance mainly diarrhea, peptic ulceration, and gastric bleeding. The analgesic effects of NSAIDs are probably linked to COX-2 inhibition, while COX-1 inhibition is the major cause of this classic adverse effects. Introduction of thiazolidinone may lead to the increase in the bulkiness leads to the preferential inhibition of COX-2 rather than COX-1 enzyme. The study aimed to synthesize derivatives of mefenamic acid with more potency and to decrease the drug's potential side effects, new series of 4-thiazolidinone derivatives of mefenamic acid were synthesized IVa-g. The synthetic procedures for target compounds and their intermediates are designed to be as follows: acylation of secondary amine of mefenamic acid by chloroacetylchloride to produce compound (I), then reaction between compound (I) and hydrazine hydrate to form hydrazine derivative of mefenamic acid (compound II). After that, Schiff base formation by addition of seven benzaldehyde derivatives and finally, cyclization in presence of thioglycolic acid to form 4-thiazolidinone heterocyclic ring. The characterization of the titled compounds has been established on the basis of their spectral FTIR, 1HNMR data, and by measurements of their physical properties. In vivo acute anti-inflammatory effect of the synthesized compounds was evaluated in rats using egg-white induced edema model of inflammation. The tested compounds and the reference drug produced significant reduction of paw edema with respect to the effect of dimethyl sulfoxide 10%v/v (control group). Compound IVe showed more potent effect than mefenamic acid at 240-300 min, while at time 300 min, compounds IVa and IVd exhibit more potent anti-inflammatory effect than mefenamic acid (50mg/kg, i.p.) as they reduced paw edema significantly more than mefenamic acid at mentioned intervals (p<0.05) . On the other hand compound IVc exhibited lower anti-inflammatory effect.

scholarly journals Anti-Inflammatory Activity and Composition ofSenecio salignusKunth

2013 ◽  
Vol 2013 ◽  
pp. 1-4 ◽  
Author(s):  
Cuauhtemoc Pérez González ◽  
Roberto Serrano Vega ◽  
Marco González-Chávez ◽  
Miguel Angel Zavala Sánchez ◽  
Salud Pérez Gutiérrez
Keyword(s):  
Medicinal Plant ◽  
Methanol Extract ◽  
Chloroform Extract ◽  
Inflammatory Activity ◽  
Paw Edema ◽  
Active Fraction ◽  
Ear Edema ◽  
Methanol Extracts ◽  
Anti Inflammatory ◽  
Inflammatory Effect

We investigated the anti-inflammatory activity ofSenecio salignus. This medicinal plant is often used in Mexico for the treatment of fever and rheumatism. Chloroform and methanol extracts of the plant were tested on 12-O-tetradecanoylphorbol-13-acetate- (TPA-) induced edema in mice ears. The methanol extract of the plant inhibited edema by36±4.4% compared with the control, while the chloroform extract exhibited an even greater level of inhibition (64.1%). The chloroform extract was then fractionated, and the composition of the active fraction was determined by GC-MS. The anti-inflammatory activity of this fraction was then tested on TPA-induced ear edema in mice, and we found that the active fraction could inhibit edema by 46.9%. The anti-inflammatory effect of the fraction was also tested on carrageenan-induced paw edema in rats at doses of 100 mg/kg; a58.9±2.8% reduction of the edema was observed 4 h after administration of carrageenan, and the effect was maintained for 5 h.

scholarly journals In Vivo Evaluation of the Anti-Inflammatory Effect ofPistacia lentiscusFruit Oil and Its Effects on Oxidative Stress

2016 ◽  
Vol 2016 ◽  
pp. 1-12 ◽  
Author(s):  
Sameh Ben Khedir ◽  
Masarra Mzid ◽  
Sana Bardaa ◽  
Dorsaf Moalla ◽  
Zouheir Sahnoun ◽  
...  
Keyword(s):  
Oxidative Stress ◽  
New Drugs ◽  
Inflammatory Activity ◽  
Natural Health Products ◽  
Paw Edema ◽  
In Vivo Evaluation ◽  
Anti Inflammatory ◽  
Fruit Oil ◽  
Inflammatory Effect

In order to find new topical anti-inflammatory agents, we had recourse to a medicinal plant. This work was designed to determine the topical anti-inflammatory effect ofPistacia lentiscusfruit oil (PLFO), using carrageenan-induced paw edema rat model, and to evaluate its effects on oxidative stress. The topical anti-inflammatory activity of PLFO was compared to Inflocine® and estimated by measuring the diameter of paw edema, for 5 hours at a 1-hour interval. After that the rats were scarified and the inflamed paw tissue was removed for the exploration of some parameters of oxidative stress and histopathology. PLFO showed a significant anti-inflammatory activity in comparison with the Inflocine. The percentages of edema inhibition were 70% and % 51.5% (p<0.01), respectively, after five hours. The treatment with PLFO and Inflocine led to significant increases (p≤0.05) in the activities of CAT, SOD, and GPX and significant decreases in the MDA level and AOPP activity in the paw tissue after Carr injection, in comparison with the Carr group. Therefore, our findings demonstrate that PLFO might accelerate the development of new drugs which could be used scientifically as a source for natural health products in the treatment of topical inflammation.

scholarly journals Antiinflammatory activity of 2-, 3-, 4-carboxymethylpyridinium hexafluorosilicates on carrageenan model of inflammation

2019 ◽  
pp. 82-87
Author(s):  
B. V. Pristupa ◽  
I. O. Shyshkin ◽  
Ya. V. Rozhkovsky ◽  
V. O. Gelmboldt
Keyword(s):  
Antiinflammatory Activity ◽  
Biologically Active ◽  
Inflammatory Activity ◽  
Male Rats ◽  
Control Group ◽  
Paw Edema ◽  
Commercial Preparation ◽  
Reference Drug ◽  
Anti Inflammatory ◽  
Inflammatory Effect

In the last decade, high cariesprophylactic efficacy of ammonium hexafluorosilicates, including salts with substituted biologically active ammonium cations, has been demonstrated. Among the promising anti-caries agents are recently synthesized 2-, 3-, 4-carboxymethylpyridinium hexafluorosilicates, for whose cations anti-inflammatory activity is expected. The aim of the work is to assess the presence of anti-inflammatory activity in the series of 2-, 3-, 4-carboxymethylpyridinium hexafluorosilicates in the experiment. 2-, 3-, 4-Carboxymethylpyridinium hexafluorosilicates (I–III, respectively) were synthesized according to the previously proposed technique, carrageenan is a commercial preparation, reference drug is a indomethacin. Experiments on the anti-inflammatory activity of hexafluorosilicates were performed on 77 white Wistar male rats weighing 174–190 g using the carrageenan model of inflammation. The inflammatory reaction was reproduced by subplantary administration of 0.1 ml of a 0.2% solution of carrageenan, the studied compounds were administered orally in doses 1/10, 1/20, 1/50 from LD50 for the compound III. It was established that after administration of carrageenan, animals of the control group showed marked paw edema, which gradually increased and was maximal after 24 hours of observation. According to the data obtained, the indices for compounds I-III practically do not differ from those of the control group. This indicates that, despite the results of the PASS forecast and the presence of acetic acid residue, an anti-inflammatory pharmacofor, in compounds I-III, the compounds under study do not have an anti-inflammatory effect in the carrageenan model. 2-, 3-, 4-Carboxymethylpyridinium hexafluorosilicates do not show the expected anti-inflammatory activity in the carrageenan model of inflammation.

scholarly journals PHYTOCHEMICAL PROFILING, FREE-RADICAL SCAVENGING AND ANTI-INFLAMMATORY ACTIVITIES OF MELIOSMA SIMPLICIFOLIA (L.)

2020 ◽  
pp. 62-68
Author(s):  
S. PAVITHR ◽  
T. SEKAR
Keyword(s):  
Free Radical ◽  
Methanol Extract ◽  
Inflammatory Activity ◽  
Scavenging Activity ◽  
Paw Edema ◽  
Stem Extract ◽  
Ft Ir ◽  
Ir Analysis ◽  
Anti Inflammatory ◽  
Dpph Scavenging

Objective: In the current research, to determine the stem extract of Meliosma simplicifolia (L.) for total phenol, tannin, total flavonoid, antioxidant activity, anti-inflammatory and identify the phytoconstituents utilizing GC-MS and FT-IR. Methods: The ability of the plant extract to act as hydrogen/electrons donor or scavenger of radicals was determined by in vitro antioxidant assays using 2,2-diphenyl-2-picryl-hydrazyl free radical (DPPH) scavenging, reducing power assay, superoxide radical (O2•) scavenging activity. The anti-inflammatory activity was evaluated using carrageenan and formalin-induced paw edema models using Wistar albino rats. The GC-MS and FT-IR analysis of the methanolic stem extract of M. simplicifolia was revealed the presence of phytochemicals. Results: Quantitative studies of estimated phenol, flavonoid and tannin, as for the methanol extract of stem showed the highest content of phenolic compounds (39.83±3.62GAE mg/100). Antioxidant activities were concluded the estimation M. simplicifolia stem for as followed the studies. In stem the methanol extract showed the highest DPPH scavenging activity (124.3µg/ml). The anti-inflammatory activity has shown in high doses of methanolic extract 250 mg/kg of significant value (p<0.05) inhibition of paw edema, on 6th hour, respectively. The FT-IR analysis has confirmed their characteristic peak values and functional groups. Conclusion: M. simplicifolia has an effective of anti-inflammatory activity and constitutes a potential source for the development of new treatments.

scholarly journals The Tea and Polysaccharide Fractions of Ximenia americana Stem Barks Inhibits Inflammatory Parameters Induced by Zymosan in Mice

2020 ◽  
Vol 11 (2) ◽  
pp. 168
Author(s):  
Gabriela Fernandes Oliveira Marques ◽  
Arcelina Pacheco Cunha ◽  
Francisco Sávio Machado Lima Gabriel ◽  
Nágila Maria Pontes Silva Ricardo ◽  
Maria Gonçalves Pereira ◽  
...  
Keyword(s):  
Acute Inflammation ◽  
Folk Medicine ◽  
Leukocyte Migration ◽  
Paw Edema ◽  
Inflammatory Parameters ◽  
Ximenia Americana ◽  
Ft Ir ◽  
Ir Analysis ◽  
Anti Inflammatory ◽  
Inflammatory Effect

Ximenia americana or “ameixa-do-sertão” is a plant used in the folk medicine of Northeast-Brazil in inflammatory and painful processes. The literature has shown anti-inflammatory and antinociceptive activities for the aqueous or hydroalcoholic extracts and polysaccharide fractions of X. americana stem barks. This study investigated the anti-inflammatory effect of polysaccharide fractions and tea prepared from X. americana stem barks in mice models of paw edema and peritonitis induced by zymosan. Tea (50,100, 150 mg/kg; p.o.) and polysaccharide fractions (FI, FII: 1 mg/kg; i.v.), containing carbohydrate (44.8, 25.0, 44.4%) and polyphenols (28.3, 0.78, 1.50%), respectively, were administered 1 h before zymosan (500 mg; s.c. or i.p). FT-IR analysis of the tea showed bands indicating C=O and C-O groups vibration, typical of phenolic compounds. Zymosan-induced paw edema (AUC: 355.0 ± 38.1) was inhibited by the tea by 38% (100 mg/kg) and 36% (150 mg/kg). FI and FII reduced the edema by 47% (933.8 ± 158.1 AUC) and 30% (1263 ± 124.8 AUC), respectively. Zymosan i.p. induced hypernociception (4.7 ± 0.3 g) and increased the peritoneal leukocyte migration (10979 ± 1475 cells/ml). FII increased by 66% the nociceptive threshold (13.87 ±1.59 g) and reduced by 63% leukocyte migration (3993 ± 439.1 cells/ml). FII decreased plasma protein by 64% (92.6 ± 4.5 vs. zymosan: 119.6 ± 5.4 mg/ml) and MDA by 63% (57.5 ± 3.5 vs. zymosan: 88.9 ± 6.3 mg/ml). The tea, containing polysaccharides and polyphenols, and polysaccharide fractions FI/FII of X. americana barks possess antiinflammatory effect in mice models of acute inflammation induced by zymosan.

scholarly journals Thiazolidin-4-one, azetidin-2-one and 1,3,4-oxadiazole derivatives of isonicotinic acid hydrazide: Synthesis and their biological evaluation

2011 ◽  
Vol 76 (8) ◽  
pp. 1057-1067 ◽  
Author(s):  
Sadaf Gilani ◽  
Suroor Khan ◽  
Ozair Alam ◽  
Vijender Singh ◽  
Alka Arora
Keyword(s):  
Lipid Peroxidation ◽  
Acid Hydrazide ◽  
Inflammatory Activity ◽  
Paw Edema ◽  
Rat Paw Edema ◽  
Anti Inflammatory ◽  
Rat Paw ◽  
New Compounds ◽  
Derivatives Of ◽  
Ulcerogenic Action

A series of thiazolidin-4-one (2a-h, 3a-h), azetidin-2-one (4a- h) and 1,3,4-oxadiazole (5a-h) derivatives of isoninicotinic acid hydrazide (INH) were synthesized in order to obtain new compounds with potential anti-inflammatory, analgesic, ulcerogenic and lipid peroxidation activities. The structures of the new compounds were supported by their IR, 1H-NMR and mass spectral data. All compounds were evaluated for their anti-inflammatory activity by the carrageenan-induced rat paw edema test method. Eleven of the new compounds, out of 32, showed very good anti-inflammatory activity in the carrageenan-induced rat paw edema test, with significant analgesic activity in the tail immersion method together with negligible ulcerogenic action. The compounds, which showed less ulcerogenic action, also showed reduced malondialdehyde content (MDA), which is one of the by-products of lipid peroxidation. The study showed that the compounds inhibited the induction of gastric mucosal lesions and it can be suggested from the results that their protective effects may be related to inhibition of lipid peroxidation in the gastric mucosa.

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