scholarly journals Synthesis of N-((2-Substituted Phenyl)-4, 5-Diphenyl-1H-Imidazol1yl)(Phenyl)Methyl) substituted amine derivatives, spectral characterization and their pharmacological evaluation

2011 ◽  
Vol 1 (5) ◽  
pp. 184-190 ◽  
Keyword(s):  
Aromatic Aldehyde ◽  
Analgesic Activity ◽  
Elemental Analysis ◽  
Spectral Characterization ◽  
Hot Plate ◽  
Pharmacological Evaluation ◽  
Paw Oedema ◽  
Anti Inflammatory ◽  
Rat Paw ◽  
Rat Paw Oedema

A series of N-((2-substituted phenyl) -4,5-diphenyl-1H-imidazol-1yl)(phenyl)methyl) substituted amine derivatives TPI (I-V) were synthesized by 2-substituted 4,5-diphenyl imidazole derivatives starting from benzyl and aromatic aldehyde. All these compounds were characterized by IR, 1HNMR, mass and elemental analysis. The newly synthesized compounds were screened for analgesic and anti-inflammatory activities by hot plate and carrageenan induced rat paw oedema methods. Compounds TPI-IV and TPI-V have showed potent anti-inflammatory activity and compounds TPI-III, TPI-IV and TPI-V showed good analgesic activity

SYNTHESIS, BIOLOGICAL EVALUATION, QSAR AND DOCKING STUDIES OF 2-AMINO-5-(SUBSTITUTED)PHENYL-1,3,4-THIADIAZOLES

INDIAN DRUGS ◽  
2015 ◽  
Vol 52 (09) ◽  
pp. 5-12
Author(s):  
S. S Mahajan ◽  
◽  
A. D. Gaitonde
Keyword(s):  
Analgesic Activity ◽  
Docking Studies ◽  
Biological Evaluation ◽  
Qsar Studies ◽  
Paw Oedema ◽  
Cox 2 ◽  
Anti Inflammatory ◽  
Analgesic Activities ◽  
Rat Paw ◽  
Rat Paw Oedema

Ten compounds from the series of 2-amino-5-(substituted)phenyl-1,3,4-thiadiazoles were synthesized and evaluated for anti-inflammatory and analgesic activities. Their structures were characterized by infrared spectroscopy and confirmed by 1H NMR spectroscopy. Anti-inflammatory activity was carried out by carrageenan-induced rat paw oedema method using indomethacin as standard. Analgesic activity was performed by acetic-acid induced writhing method in mice using aspirin as standard. The QSAR studies were performed for the analgesic activity using the software ‘Strike’ from Schrodinger. Docking studies were carried out for COX-2 inhibition using the software ‘Glide’ from Schrodinger. The compounds were obtained in good yields and possessed good anti-inflammatory and analgesic activities. Various physicochemical parameters, contributing towards analgesic activity were identified from the QSAR studies. The Glide Scores were more or less correlated with the anti-inflammatory and analgesic activities of compounds.

scholarly journals Synthesis, characterization and pharmacological evaluation of substituted phenoxy acetamide derivatives

2015 ◽  
Vol 69 (4) ◽  
pp. 405-415 ◽  
Author(s):  
Priyanka Rani ◽  
Dilip Pal ◽  
Rahul Hegde ◽  
Syed Hashim
Keyword(s):  
Analgesic Activity ◽  
Diclofenac Sodium ◽  
Inflammatory Activity ◽  
The Novel ◽  
Standard Drug ◽  
Antipyretic Activity ◽  
Paw Oedema ◽  
Anti Inflammatory ◽  
Rat Paw ◽  
Rat Paw Oedema

A novel series of 2-(substituted phenoxy)-N-(1,7,7-trimethylbicyclo[2.2.1]heptan-2-yl)acetamide and N-(2-bromocyclohexyl)-2-(substituted phenoxy)acetamide derivatives having cyclohexyl nucleus as common in both types were synthesized and assessed for their anti-inflammatory activity by a carrageenan induced rat paw oedema method, analgesic activity by Eddy?s hot plate method and antipyretic activity by brewer?s yeast induced pyrexia method. All the novel derivatives have been synthesized by the reaction of camphor and similar ketone having cyclohexane nucleus (e.g. 2-bromocyclohexanone) with ammonium carbonate and formic acid resulting in the formation of aromatic amines (1a-b). These amines on further chloroacetylation with chloroacetylchloride give compounds (2a-b). Compounds (2a-b) are converted to 2-(substituted phenoxy)-N-(1,7,7-trimethylbicyclo[2.2.1]heptan-2-yl) acetamide and N-(2-bromocyclohexyl)-2-(substituted phenoxy)acetamide derivatives on treatment with substituted phenol. Among the series 3a-f, 3i, 3k, 3l compounds showed significant anti-inflammatory activity as compared to the standard drug diclofenac sodium and also compound 3a-f, 3h, 3j, 3k exhibit significant analgesic activity as compared to the standard drug. Compounds 3a-f and 3k showed antipyretic activity nearly to the standard drug indomethacin. Compounds 3a-f and 3k possess anti-inflammatory, analgesic and antipyretic activities near to the standard.

scholarly journals Antinociceptive and Anti-Inflammatory Activities of Leaf Methanol Extract ofCotyledon orbiculataL. (Crassulaceae)

2012 ◽  
Vol 2012 ◽  
pp. 1-6 ◽  
Author(s):  
George J. Amabeoku ◽  
Joseph Kabatende
Keyword(s):  
Acetic Acid ◽  
Reaction Time ◽  
Plant Species ◽  
Methanol Extract ◽  
Thermal Stimulation ◽  
Hot Plate ◽  
Paw Oedema ◽  
Anti Inflammatory ◽  
Rat Paw ◽  
Rat Paw Oedema

Leaf methanol extract ofC. orbiculataL. was investigated for antinociceptive and anti-inflammatory activities using acetic acid writhing and hot-plate tests and carrageenan-induced oedema test in mice and rats, respectively.C. orbiculata(100–400 mg/kg, i.p.) significantly inhibited acetic acid-induced writhing and significantly delayed the reaction time of mice to the hot-plate-induced thermal stimulation. Paracetamol (300 mg/kg, i.p.) significantly inhibited the acetic acid-induced writhing in mice. Morphine (10 mg/kg, i.p.) significantly delayed the reaction time of mice to the thermal stimulation produced with hot plate. Leaf methanol extract ofC. orbiculata(50–400 mg/kg, i.p.) significantly attenuated the carrageenan-induced rat paw oedema. Indomethacin (10 mg/kg, p.o.) also significantly attenuated the carrageenan-induced rat paw oedema. The LD50value obtained for the plant species was greater than 4000 mg/kg (p.o.). The data obtained indicate thatC. orbiculatahas antinociceptive and anti-inflammatory activities, justifying the folklore use of the plant species by traditional medicine practitioners in the treatment of painful and inflammatory conditions. The relatively high LD50obtained shows thatC. orbiculatamay be safe in or nontoxic to mice.

Fibrinolytic, Anti-Inflammatory and Cytotoxic Potentialities of Extracts and Chemical Constituents of Manglicolous Lichen, Graphis ajarekarii Patw. & C. R. Kulk

2020 ◽  
Vol 10 (1) ◽  
pp. 87-93 ◽  
Author(s):  
Vinay Bharadwaj Tatipamula ◽  
Girija Sastry Vedula
Keyword(s):  
Protein Denaturation ◽  
Biological Activities ◽  
Chemical Constituents ◽  
Fibrin Clot ◽  
Hydroalcoholic Extract ◽  
Paw Oedema ◽  
Anti Inflammatory ◽  
Rat Paw ◽  
Rat Paw Oedema

Background: Lichens which are betide to mangroves are termed as Manglicolous Lichens (ML). As these ML are habituated under stress conditions, they are screened for unique metabolites and biological activities. Objective: The study aimed to establish the chemical and biological profile of ML, Graphis ajarekarii. Methods: The Ethyl Acetate Extract of G. ajarekarii (EAE) was subjected to chromatographic techniques and the obtained isolates were characterized by spectroscopic analysis. The hydroalcoholic extract of G. ajarekarii (AE), EAE, isolates and Hydroalcoholic Extract of host (HE) were evaluated for fibrinolytic (fibrin clot method), in vitro (protein denaturation method) and in vivo (formalin-induced rat paw oedema assay), anti-inflammatory and cytotoxicity (MTT assay) activities. Results: Chemical investigation of the EAE led to the isolation of two known compounds namely atranorin (1) and ribenone (2), which were confirmed by spectral data. The AE and EAE gradually lysed the fibrin clot with 94.54 and 65.07%, respectively, at 24 h. The AE inhibited protein denaturation of about 88.06%, while the standard (Indomethacin) with 93.62%. Similarly, the in vivo antiinflammatory analysis of AE (200 mg/mL) showed potent reduction of rat paw oedema than the standard, whereas EAE and 1 depicted moderate depletion. In addition, the AE revealed prominence inhibition on MCF-7, DU145 and K-562 with IC50 values of 69.5, 42.5 and 38 µg/mL, respectively, whereas the HE exhibited mild inhibitory profile against fibrin clot, inflammation and cancer. Conclusion: From the results, it can be concluded that the G. ajarekarii has an aptitude to act against coagulation, inflammation and cancer cells.

Anti-Inflammatory Constituents of Alchornea cordifolia Leaves

2015 ◽  
Vol 19 ◽  
pp. 60-64
Author(s):  
AA Ahmadu ◽  
A Agunu ◽  
EM Abdurrahman
Keyword(s):  
Medicinal Plant ◽  
West Africa ◽  
Ethyl Acetate ◽  
Leaf Extract ◽  
Methyl Gallate ◽  
Paw Oedema ◽  
Analgesic Agents ◽  
Anti Inflammatory ◽  
Rat Paw ◽  
Rat Paw Oedema

Alchornea cordifolia (Schum and Thonn) Muell. Arg. (Euphorbiaceae) is a traditional medicinal plant widely distributed in West Africa including Nigeria.The plant has been used for ethnomedicinal purposes against wounds, ulcers, and sores. The decoction of the leaves has been reported to provide remedies for bronchial problems, rheumatic pain and cough. From the dichloromethane and ethyl acetate soluble parts of the Methanol leaf extract, two compounds namely Lup-20(29)-en-3c-ol (lupenol) and Methyl 3, 4,5-trihydroxy benzoate (Methyl gallate) were isolated and their structures elucidated. Anti-inflammatory and analgesic properties of the compounds on carrageenan-induced paw oedema and formalin-induced pain in rats showed that compound 2 significantly (P<0.05) inhibit rat paw oedema compared to the standard drugs (Piroxicam and Morphine) used, while on formalin-induced pain in rats, the same trend was observed and were both comparable to Piroxicam and morphine, the standard anti-inflammatory and analgesic agents used, respectively. Compound 1 did not show any significant anti-inflammatory activity compared to control, likewise compound 2. Thus, compound 2, Methyl trihydroxy benzoate, might be responsible for the anti-inflammatory and analgesic properties of this plant.Keywords: Alchornea cordifolia, Anti-inflammatory, Analgesic, Methyl Trihydroxy Benzoate

scholarly journals A New Cytotoxic Sesquiterpene and Three Anti-inflammatory Flavonoids from Egyptian Tanacetum Santolinoides

2007 ◽  
Vol 2 (11) ◽  
pp. 1934578X0700201 ◽  
Author(s):  
Sabrin R. M. Ibrahim ◽  
Jihan M. Badr ◽  
Khalid A. El Sayed ◽  
Diaa T. A. Youssef
Keyword(s):  
Cytotoxic Activity ◽  
Brine Shrimp ◽  
Methanolic Extract ◽  
Spectral Characteristics ◽  
Mass Spectral ◽  
Aerial Parts ◽  
Paw Oedema ◽  
Anti Inflammatory ◽  
Rat Paw ◽  
Rat Paw Oedema

A re-investigation of the methanolic extract of the aerial parts of Tanacetum santolinoides has resulted in the isolation of a new sesquiterpene, tanacetonic acid (1), along with three known methoxylated flavonoids. The structure of the isolated compounds was secured based on their IR, UV, 1D and 2D (1H-1H COSY, HSQC and HMBC) NMR spectroscopic and FAB mass spectral characteristics. The new sesquiterpene showed a significant cytotoxic activity when tested using the brine shrimp bioassay, while the three flavonoids demonstrated anti-inflammatory effects in the rat paw oedema test.

scholarly journals Anti-Inflammatory Activity of Pleurotus ostreatus, a Culinary Medicinal Mushroom, in Wistar Rats

2020 ◽  
Vol 2020 ◽  
pp. 1-9
Author(s):  
W. J. A. Banukie N. Jayasuriya ◽  
Shiroma M. Handunnetti ◽  
Chandanie A. Wanigatunge ◽  
Gita H. Fernando ◽  
D. Thusitha U. Abeytunga ◽  
...  
Keyword(s):  
Pleurotus Ostreatus ◽  
Inflammatory Activity ◽  
No Production ◽  
Protective Effects ◽  
Paw Oedema ◽  
Freeze Dried ◽  
Anti Inflammatory ◽  
Rat Paw ◽  
Rat Paw Oedema

Context. Pleurotus ostreatus (P.o) is a culinary mushroom which is commonly called as “oyster mushroom” belonging to the Basidiomycetous fungi of the order Agaricales and family Pleurotaceae. Objectives. The present study investigates the anti-inflammatory potential of P.o and the underlying mechanisms of activity. Materials and Methods. Anti-inflammatory activity was evaluated using suspensions of freeze-dried and powdered (SFDP) P.o and acetone extract (AE) of P.o in normal and alloxan-induced diabetic rats using the carrageenan-induced rat paw oedema model. The mechanisms by which P.o is mediating the anti-inflammatory activity were studied using in vivo and in vitro assays. Results. At doses of 500–1000 mg/kg, the SFDP of P.o showed long-lasting activity at both early and late phases of carrageenan-induced rat paw oedema. The dose of 750 mg/kg showed the most potent inhibitory activity (92% inhibition) in healthy rats. The AE of P.o showed maximum inhibition of oedema of 87%. P.o exerted protective effects on the inflammatory pathologies in rats with diabetes. The possible mechanisms by which P.o mediates the anti-inflammatory activity were antihistamine activity (52.1%), inhibition of cell migration to the site of inflammation (45.4%), in vitro membrane stabilizing activity (52.6%), and inhibition of nitric oxide (NO) production (91.2%) (P<0.05). Dose-dependent inhibition of NO production was seen with in vitro treatment of rat peritoneal cells with AE of P.o (r = 0.95; P<0.05). Discussion and Conclusion. The promising activity of culinary mushroom P.o against inflammation suggests its potential application as a functional food during inflammatory conditions.

scholarly journals Synthesis and Evaluation of New Coumarin Derivatives as Antioxidant, Antimicrobial, and Anti-Inflammatory Agents

Molecules ◽  
2020 ◽  
Vol 25 (14) ◽  
pp. 3251 ◽  
Author(s):  
Hanan M. Alshibl ◽  
Ebtehal S. Al-Abdullah ◽  
Mogedda E. Haiba ◽  
Hamad M. Alkahtani ◽  
Ghada E.A. Awad ◽  
...  
Keyword(s):  
Significant Inhibition ◽  
Coumarin Derivatives ◽  
Paw Oedema ◽  
Cox 2 ◽  
Anti Inflammatory ◽  
Rat Paw ◽  
Orally Active ◽  
Rat Paw Oedema ◽  
Sulfonamide Compound

New pyranocoumarin and coumarin-sulfonamide derivatives were prepared and evaluated for their antioxidant, antimicrobial, and/or anti-inflammatory activities. Coumarin-sulfonamide compounds 8a–d demonstrated significant antioxidant activity, while 7c,d, 8c,d, and 9c,d exhibited antimicrobial activity equal to or higher than the standard antimicrobials against at least one tested microorganism. Regarding the anti-inflammatory testing, pyranocoumarins 2b, 3a,b and 5c and coumarin-sulfonamide compound 9a showed more potent antiproteinase activity than aspirin in vitro; however, five compounds were as potent as aspirin. The anti-inflammatory activity of the promising compounds was further assessed pharmacologically on formaldehyde-induced rat paw oedema and showed significant inhibition of oedema. For in vitro COX-inhibitory activity of coumarin derivatives, pyranocoumarin derivative 5a was the most selective (SI = 152) and coumarin-sulfonamide derivative 8d was most active toward COX-2 isozyme. The most active derivatives met the in silico criteria for orally active drugs; thus, they may serve as promising candidates to develop more potent and highly efficient antioxidant, antimicrobial, and/or anti-inflammatory agents.

scholarly journals Analgesic and Toxicity Studies of Aminoacetylenic Isoindoline-1,3-dione Derivatives

2012 ◽  
Vol 2012 ◽  
pp. 1-8 ◽  
Author(s):  
Raghad Shakir ◽  
Zuhair A. Muhi-eldeen ◽  
Khalid Z. Matalka ◽  
Nidal A. Qinna
Keyword(s):  
Oral Administration ◽  
Analgesic Activity ◽  
Positive Control ◽  
Gastric Lesions ◽  
Paw Edema ◽  
Hot Plate ◽  
Rat Paw Edema ◽  
Ulcerogenic Activity ◽  
Anti Inflammatory ◽  
Rat Paw

We have developed a series of aminoacetylenic isoindoline-1,3-dione compounds and showed their anti-inflammatory activities by reducing carrageenan-induced rat paw edema and modulating proinflammatory and anti-inflammatory cytokines. In the present study and due to efficacy reasons, we are exploring only two of these compounds, namely, ZM4 and ZM5, to reveal their analgesic activity and toxicity. Following oral administration, both compounds were effective in reducing significantly (P<0.05–0.001) acetic acid-induced writhing behavior, hot plate latency test, and formalin-induced paw licking time as antinociceptive indicators in mice and rats, respectively. Regarding the toxicity, the acute (20, 50, and 150 mg/kg) and repeated oral administration (10, 20, and 50 mg/kg) of these compounds for ten days did not produce any mortality and the compounds were considered well tolerated. However, repeated oral administration of 50 mg/kg of both compounds induced erythropoiesis by means of increasing significantly red blood cells, hemoglobin, and packed cell volume. Moreover, these compounds did not induce gastric lesions in the stomach of experimental animals at the doses that exhibited analgesic and anti-inflammatory activity compared to indomethacin as a positive control. The results indicate that ZM4 and ZM5 possess potential analgesic activity while being preliminarily safe and have minimal ulcerogenic activity.

scholarly journals Anti-inflammatory and Anti-arthritic Activities ofMerremia tridentate(L.) Hall. f.

2009 ◽  
Vol 6 (4) ◽  
pp. 943-948 ◽  
Author(s):  
M. Kamalutheen ◽  
S. Gopalakrishnan ◽  
T. Syed Ismail
Keyword(s):  
Ethanol Extract ◽  
Albino Rats ◽  
Standard Drug ◽  
Arthritis Model ◽  
Paw Oedema ◽  
Dependent Activity ◽  
Anti Inflammatory ◽  
Rat Paw ◽  
Dose Dependent ◽  
Rat Paw Oedema

The various extracts ofMerremia tridentatewere investigated for its anti-inflammatory and anti-arthritic activities in male albino rats. The anti-inflammatory activity was carried out using carrageenan-induced rat paw oedema model and the anti-arthritic activity was carried out using complete Freund’s adjuvant induced arthritis model. Indomethacin (10 mg/kg bw) was used as a standard drug. The ethanol extract ofM. tridentateexhibited significant dose dependent activity in acute inflammation and the doses of 100 mg/kg bw and 200 mg/kg bw produced 38.3% and 42.8% inhibition respectively after 3 h as compared with that of the standard drug which showed 48.5% inhibition. In arthritis model, the doses of 100 mg/kg bw and 200 mg/kg bw of the ethanol extract produced 49.0% and 51.7% inhibition respectively after 19 days when compared with that of the standard drug (55.5%). Both doses of the ethanol extract ofM. tridentateexhibit significant anti-inflammatory and anti-arthritic activities.

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