scholarly journals Synthesis and Anti-inflammatory Activity of Some Novel Pyrazole Derivatives of Gallic Acid

2009 ◽  
Vol 6 (s1) ◽  
pp. S123-S128 ◽  
Author(s):  
S. Arunkumar ◽  
K. Ilango ◽  
R. S. Manikandan ◽  
N. Ramalakshmi
Keyword(s):  
Sodium Hydroxide Solution ◽  
Aromatic Aldehydes ◽  
Inflammatory Activity ◽  
Pyrazole Derivatives ◽  
Paw Edema ◽  
Mass Spectral Data ◽  
Mass Spectral ◽  
Anti Inflammatory ◽  
Derivatives Of

In the present study, a new series of [5-substituted-3-(phenylamino)-1H-pyrazol-1yl] (3,4,5-trihydroxyphenyl)-methanone (4a-j) have been synthesized. 3, 4, 5-Trihydroxy benzohydrazide (1) was synthesized from propyl gallate and hydrazine hydrate in presence of ethanol. Chalcones (2a-j) were synthesized from acetanilide and various aromatic aldehydes in presence of ethanol and sodium hydroxide solution. By refluxing the compound (1) and compounds (2a-j) in presence of ethanol yielded [5-substituted-3-(phenylamino)-4.5-dihydropyrazol-1yl] (3,4,5-trihydroxy phenyl)-methanone (3a-j). The final compounds [5-substituted-3-(phenylamino)-1H-pyrazol-1yl] (3,4,5-trihydroxyphenyl)-methanone (4a-j) were synthesized by treating compounds (3a-j) with bromine water. The synthesized compounds have been characterized by IR,1HNMR and Mass spectral data. The compounds were evaluated forin vivoanti-inflammatory activity by carrageenan induced paw edema test. In general all compounds were found to exhibit good anti-inflammatory activity.

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 and Anti-inflammatory Activity of Some Novel 2,4-Diaryl-3,5-bis(arylimino)-1,2,4-thiadiazolidine Derivatives

2009 ◽  
Vol 6 (2) ◽  
pp. 495-503 ◽  
Author(s):  
P. Venkatesh ◽  
S. N. Pandeya
Keyword(s):  
Diclofenac Sodium ◽  
Inflammatory Activity ◽  
Second Step ◽  
Paw Edema ◽  
Mass Spectral Data ◽  
Mass Spectral ◽  
Methoxy Groups ◽  
Anti Inflammatory ◽  
Sar Study ◽  
New Compounds

A series of some novel 2,4-diaryl-3,5-bis(arylimino)-1,2,4-thiadiazolidine derivatives were synthesized and evaluated for anti-inflammatory activity. In the SAR study, the phenyl ring on 3 and 4 position of 1,2,4-thiadiazolidine ring substituted with chloro, nitro and methoxy groups showed better activity. The title compounds were synthesized from two steps; the first step involved the synthesis of diaryl substituted thioureas then, it was cyclised to give the 1,2,4-thiadiazole system in the presence of oxidizing agent (hydrogen peroxide and concentrated hydrochloric acid) in the second step. The purity of the synthesized compounds were judged by their C, H and N analysis and the structure was analyzed on the basis of IR, H1NMR, C13NMR and Mass spectral data. The anti-inflammatory activity of new compounds was determined by λ-Carrageenan induced mice paw edema method using diclofenac sodium as a standard. Among the compounds tested four compounds, B2 (2,4-diphenyl-3,5-bis(3-nitrophenylimino)-1,2,4-thiadiazolidine), B4 (2,4-diphenyl-3,5-bis(3-chlorophenylimino)-1,2,4-thiadiazolidine), B6 (2,4-diphenyl-3,5-bis(4-methoxyphenylimino)-1,2,4-thiadiazolidine) and B7 (2,4-diphenyl-3,5-bis (2-methoxyphenylimino)-1,2,4-thiadiazolidine) were the most active compounds in these series.

ANTIULCER AND ANTI-INFLAMMATORY ACTIVITIES OF HYDROALCOHOLIC EXTRACTS OF STEM BARK AND LEAF OF ANOGEISSUS PENDULA EDGEW

INDIAN DRUGS ◽  
2021 ◽  
Vol 58 (01) ◽  
pp. 41-46
Author(s):  
Deeksha Singh ◽  
◽  
Amit Nayak ◽  
Rakesh Yadav ◽  
Uttam Singh Baghel ◽  
...  
Keyword(s):  
Phenolic Compounds ◽  
Stem Bark ◽  
Inflammatory Activity ◽  
Antiulcer Activity ◽  
Paw Edema ◽  
Ulcer Index ◽  
Pylorus Ligation ◽  
Anti Inflammatory ◽  
Anogeissus Pendula

Anogeissus pendula Edgew has been reported to be used in gastric disorder even though no attempt has been made to evaluate the same. The present study was designed to evaluate the hydroalcoholic extracts of stem bark and leaves for in vivo acute antiulcer and anti-inflammatory activities. Antiulcer activity was studied by pylorus ligation induced ulcers while anti-inflammatory activities was studied by carrageenan induced paw edema. The extract of stem bark at 200 and 400 mg/kg b. w., significantly (P<0.05) reduced ulcer index whereas extracts of both stem bark and leaves significantly (P<0.001) reduced paw diameter at the fifth hour. The hydroalcholic extract of stem bark of A. pendula possesses more significant antiulcer and anti-inflammatory activity than the hydroalcholic extract of leaves may be due to the presence of higher amount of phenolic compounds.

In vitro and in vivo delivery of atorvastatin: A comparative study of anti-inflammatory activity of atorvastatin loaded copolymeric micelles

2017 ◽  
Vol 32 (8) ◽  
pp. 1127-1138 ◽  
Author(s):  
Sina Andalib ◽  
Pezhman Molhemazar ◽  
Hossein Danafar
Keyword(s):  
Inflammatory Responses ◽  
Inflammatory Activity ◽  
Lipid Lowering ◽  
Precipitation Method ◽  
Paw Edema ◽  
Scanning Calorimetry ◽  
Rat Paw Edema ◽  
Anti Inflammatory

Statins have been shown to exert ‘pleiotropic effects’ independent of their cholesterol lowering actions that include anti-inflammatory properties. In this study we synthesized mono methoxy poly (ethylene glycol)–poly (ε-caprolactone) (mPEG-PCL) di block copolymers. The structure of the copolymers was characterized by H nuclear magnetic resonance, Fourier-transform infrared spectroscopy, differential scanning calorimetry and gel permeation chromatography techniques. In this method, atorvastatin was encapsulated within micelles through a single-step nano-precipitation method, leading to the formation of atorvastatin-loaded mPEG-PCL (atorvastatin/mPEG-PCL) micelles. The resulting micelles were characterized further by various techniques such as dynamic light scattering and atomic force microscopy. In this study the anti-inflammatory activity of atorvastatin and atorvastatin/mPEG-PCL micelles on acute models of inflammation are analyzed, to compare the effect of indometacin in rats. Carrageenan induces rat paw edema; six animals of each group (10 groups) received indometacin, atorvastatin, and atorvastatin/mPEG-PCL micelles orally 1, 6, 12 and 24 h before carrageenan injection in paw. The paw edema thickness measured at 1, 2, 3 and 4 h after injection and percentage inhibition of edema in various groups were calculated. The results showed that the zeta potential of micelles was about −16.6 mV and the average size was 81.7 nm. Atorvastatin was encapsulated into mPEG-PCL micelles with loading capacity of 14.60 ± 0.96% and encapsulation efficiency of 62.50 ± 0.84%. Atorvastatin and atorvastatin/mPEG-PCL micelles showed significant anti-inflammatory activity in the present study. The anti-inflammatory activity of atorvastatin and atorvastatin/mPEG-PCL micelles was significant in comparison with indometacin. Atorvastatin/mPEG-PCL micelles showed more anti-inflammatory activity than atorvastatin. This study revealed the anti-inflammatory activity of atorvastatin and atorvastatin/mPEG-PCL micelles and suggested the statins have a potential inflammatory activity along with its lipid lowering properties. Contrary to anti-inflammatory effects, the pro-inflammatory responses are independent of 3-hydroxy-3-methylglutaryl coenzyme A reductase inhibition and can be mediated directly by atorvastatin.

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 Quinazoline-containing Hydrazydes of Dicarboxylic Acids and Products of Their Structural Modification: A Novel Class of Anti-inflammatory Agents

2021 ◽  
Vol 68 (2) ◽  
pp. 395-403
Author(s):  
Nataliia Krasovska ◽  
Viktor Stavytskyi ◽  
Inna Nosulenko ◽  
Oleksandr Karpenko ◽  
Oleksii Voskoboinik ◽  
...  
Keyword(s):  
Chemical Modification ◽  
Spectral Data ◽  
1H Nmr ◽  
Structural Modification ◽  
Dicarboxylic Acids ◽  
Inflammatory Activity ◽  
Mass Spectral Data ◽  
Mass Spectral ◽  
Anti Inflammatory ◽  
Amide Fragment

The synthesis of hydrazides formed by quinazolin-4(3H)-ylidenehydrazine and dicarboxylic acids, as well as their further modification are described in the present manuscript. It was shown that above-mentioned hydrazides may be obtained via acylation of initial quinazolin-4(3H)-ylidenehydrazine by corresponding acylhalides, cyclic anhydrides and imidazolides of dicarboxylic acids monoesters. Obtained hydrazides were converted into [1,2,4]triazolo[1,5-с]quinazolines that were used as initial compounds for chemical modification aimed to the introduction of amide fragment to the molecule. The IR, 1H NMR and chromato-mass spectral data of obtained compounds were studied and discussed. Obtained substances were studied for anti-inflammatory activity using carrageenan-induced paw inflammation model. Amides of ([1,2,4]triazolo[1,5-с]quinazoline-2-yl)alkyl carboxylic acids were detected as promising class of anti-inflammatory agents for further purposeful synthesis and profound study of anti-inflammatory activity.

scholarly journals Synthesis, Anti-inflammatory Activity and in silico Studies of Some Novel Morpholine Based Carboxamides

2020 ◽  
Vol 32 (4) ◽  
pp. 901-906
Author(s):  
Premanand M. Honavar ◽  
Vasantha Kumar ◽  
P. Nikhil ◽  
Naveen Kumar ◽  
S. Sreenivasa ◽  
...  
Keyword(s):  
Inflammatory Activity ◽  
Mass Spectral Data ◽  
Mass Spectral ◽  
Rat Paw Edema ◽  
Amide Derivatives ◽  
In Silico Studies ◽  
Anti Inflammatory ◽  
Docking Interaction ◽  
Rat Paw ◽  
Aromatic Heterocyclic

Two series of carboxamides were synthesized from 3-fluoro-4-morpholinoaniline and different substituted aromatic/heterocyclic carboxylic acids. All the compounds were characterized by IR, 1H NMR, 13C NMR and mass spectral data. The newly synthesized amide derivatives were screened for anti-inflammatory activity by following carrageenan induced rat paw edema method. Among the compounds screened, compound 6e was found to be highly potent. Molecular docking interaction of active compounds revealed that effective binding was observed in the pocket of COX-I and COX-II proteins.

Inhibition of iNOS by Benzimidazole Derivatives: Synthesis, Docking, and Biological Evaluations

2021 ◽  
Vol 17 ◽  
Author(s):  
Richa Minhas ◽  
Yogita Bansal
Keyword(s):  
Inflammatory Activity ◽  
Benzimidazole Derivatives ◽  
Critical Study ◽  
Paw Edema ◽  
Rat Paw Edema ◽  
Anti Inflammatory ◽  
Inos Inhibitors ◽  
Rat Paw

Background: Inducible nitric Oxide Synthase (iNOS) plays a key role in the progression of inflammatory diseases by accelerating the production of NO, which makes it an intriguing target to treat inflammation in complex diseases. Therefore, the search is on to develop molecules as selective iNOS inhibitors. Objective: The present work was aimed to design, synthesize and evaluate benzimidazole-coumarin coupled molecules as anti-iNOS agents through in silico and pharmacological studies. Methods: A critical study of literature reports on iNOS inhibitors led to the selection of a (un)substituted coumarin nucleus, 2-aminobenzimidazole, and a 4-atom linker as important structural components for iNOS inhibition. Two series of compounds (7-16 and 17-26) were designed and synthesized by coupling these components. The compounds were subjected to docking using iNOS (1QW4) and nNOS (1QW6) as targets. All compounds were evaluated for NO and iNOS inhibitory activities in vitro. The selected compound was finally evaluated for anti-inflammatory activity in vivo using the carrageenan-induced rat paw edema model. Results : All compounds showed moderate to good inhibition of NO and iNOS in vitro. Compound 12 was the most potent inhibitor of NO and iNOS. Hence, it was evaluated in vivo for toxicity and anti-inflammatory activity. It was found to be safe in acute toxicity studies, and effective in reducing the rat paw edema significantly. Its anti-inflammatory behaviour was similar to that of aminoguanidine, which is a selective iNOS inhibitor. Conclusion: The newly synthesized benzimidazole-coumarin hybrids may serve as potential leads for the development of novel anti-iNOS agents.

SYNTHESIS, DOCKING STUDY AND ANTI-INFLAMMATORY STUDIES OF SOME FLAVANONES

INDIAN DRUGS ◽  
2021 ◽  
Vol 58 (02) ◽  
pp. 54-60
Author(s):  
Ishwar K. Bhat ◽  
Keyword(s):  
Diclofenac Sodium ◽  
Docking Study ◽  
Inflammatory Activity ◽  
Mass Spectral Data ◽  
Ligand Interaction ◽  
Standard Drug ◽  
Mass Spectral ◽  
H Nmr ◽  
Anti Inflammatory ◽  
Phosphoinositide 3 Kinase

In this work, a series of flavanones (P1-P9) was synthesized by cyclization of substituted (hydroxyphenyl)- 3-(phenyl) prop-2-en-1-ones (S1-S9). The structures of the synthesized compounds were characterized by IR, 1 H NMR and mass spectral data. These derivatives were evaluated for anti-inflammatory activity. Compounds P1, P3, P6 and P7 showed excellent anti-inflammatory activity as compared to standard drug diclofenac sodium. Molecular docking of these flavanones (P1-P9) was also performed with receptor phosphoinositide-3-kinase PI3Kδ (PDB code: 5ITD). All the flavanones (P1-P9) were docked into same groove of the binding site of native co-crystallized (5-{4-[3-(4-acetylpiperazine-1-carbonyl) phenyl] quinazolin-6-yl}-2-methoxypyridine carbonitrile) ligand for activity explanation and exhibited good ligand interaction and binding affinity were of range -4.57 to -8.79kcal/mol.

scholarly journals Synthesis, reactions and biological activity of 3-arylidene-5-(4-methylphenyl)-2(3H)-furanones?

2009 ◽  
Vol 74 (2) ◽  
pp. 103-115 ◽  
Author(s):  
Asif Husain ◽  
Mumtaz Alam ◽  
Nadeem Siddiqui
Keyword(s):  
Aromatic Aldehydes ◽  
Antibacterial Activities ◽  
Inflammatory Activity ◽  
Writhing Test ◽  
Mass Spectral ◽  
Rat Paw Edema ◽  
Anti Inflammatory ◽  
Rat Paw ◽  
New Compounds ◽  
Synthesis Reactions

3-Arylidene-5-(4-methylphenyl)-2(3H)-furanones 2a-m were prepared from 3-(4-methyl-benzoyl)propanoic acid 1 and several aromatic aldehydes. Some of the selected furanones were reacted with ammonia gas and benzylamine to give corresponding 3-arylidene-1,3-dihydro-5-(4-methylphenyl)-2H-pyrrol- 2-ones 3a-h and 3-arylidene-1-benzyl-1,3-dihydro-5-(4-methylphenyl)-2H- -pyrrol-2-ones 4a-f, respectively, which were characterized on the basis of IR, 1H-NMR, mass spectral data and elemental analysis results. These compounds were tested for their anti-inflammatory and antibacterial activities. The compounds, which showed significant anti-inflammatory activity, were further screened for their analgesic and ulcerogenic activities. Three new compounds (2e, 2h and 4d), out of twenty-seven showed very good anti-inflammatory activity in the carrageenan induced rat paw edema test, with significant analgesic activity in the acetic acid induced writhing test together with negligible ulcerogenic action. The antibacterial activity is expressed as the corresponding MIC values.

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