scholarly journals Design and Synthesis of 7-Chloro-3-Substituted Quinazolin-4(3H)-Ones as Potential Anti-inflammatory and Analgesic Agents

2017 ◽  
Vol 9 (05) ◽  
Author(s):  
Arun Mahato ◽  
Birendra Shrivastava ◽  
Nithya Shanthi
Keyword(s):  
Spectroscopic Studies ◽  
Tail Flick ◽  
Preliminary Evaluation ◽  
Significant Activity ◽  
Design And Synthesis ◽  
Paw Oedema ◽  
Analgesic Agents ◽  
Anti Inflammatory ◽  
Rat Paw ◽  
Quinazolinone Derivatives

In our effort to identify potent anti-inflammatory and analgesic agents a number of 7-chloro-3-substituted-2-phenylquinazolin-4(3H)-ones have been synthesized starting from 4-chloro anthranilic acid. Docking analysis of the quinazolinone derivatives were done with COX-II protein which was carried out by means of the AutoDock program. Their structures have been elucidated on the basis of elemental analyses and spectroscopic studies (IR, 1H-NMR, MS). The synthesized compounds were tested for their analgesic activity by tail-flick method and anti-inflammatory activity by carrageenan induced rat paw oedema method. Preliminary evaluation of the anti-inflammatory and analgesic properties of the prepared compounds has indicated that some of them exhibit moderate to significant activity, compared to diclofenac standard.

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

Synthesis of novel thiadiazole derivatives as selective COX-2 inhibitors

MedChemComm ◽  
2016 ◽  
Vol 7 (12) ◽  
pp. 2309-2327 ◽  
Author(s):  
Fatma A. Ragab ◽  
Helmi I. Heiba ◽  
Marwa G. El-Gazzar ◽  
Sahar M. Abou-Seri ◽  
Walaa A. El-Sabbagh ◽  
...  
Keyword(s):  
Paw Oedema ◽  
Analgesic Agents ◽  
Thiadiazole Derivatives ◽  
Cox 2 ◽  
Anti Inflammatory ◽  
Rat Paw ◽  
Cox 2 Inhibitors ◽  
Rat Paw Oedema

A novel series of thiadiazole derivatives were designed and synthesized for evaluation as selective COX-2 inhibitors in vitro and were investigated in vivo as anti-inflammatory and analgesic agents against carrageenan-induced rat paw oedema model in irradiated rats.

scholarly journals DESIGN AND SYNTHESIS OF NOVEL 4-(4-FLUORO-3-METHYLPHENYL)-6-(SUBSTITUTED ARYL)-1,6-DIHYDROPYRIMIDIN-2-OL DERIVATIVES AS POTENT ANTI-INFLAMMATORY AND ANALGESIC AGENTS

2019 ◽  
pp. 251-256
Author(s):  
MURALIDHARAN V ◽  
RAJA S ◽  
ASHA DEEPTI
Keyword(s):  
Pyrimidine Derivative ◽  
Cellular Level ◽  
Tail Flick ◽  
Design And Synthesis ◽  
Rat Paw Edema ◽  
Analgesic Agents ◽  
Anti Inflammatory ◽  
Analgesic Activities

Objective: Pyrimidine heterocycles possessing hydroxy group has a unique place in medicinal chemistry and also plays a key role in biological processes. In the biological functions at cellular level pyrimidine plays imperative roles which lead the researchers to design a variety of its derivatives. The aim of the present study was to synthesize the novel set of 4-(4-fluoro-3-methylphenyl)-6-(substituted aryl)-1,6-dihydropyrimidin-2-ol derivatives. These compounds were screened for their analgesic and anti-inflammatory activities. Methods: A novel series of 4-(4-fluoro-3-methylphenyl)-6-(substituted aryl)-1,6-dihydro pyrimidin-2-ol derivatives were furnished in two steps starting from 4-fluoro-3-methyl acetophenone through chalcone formation. Human red blood cell membrane stabilization method and carrageenan-induced rat paw edema test were performed for screening in vitro and in vivo anti-inflammatory activity, respectively. Tail-flick technique was performed for screening analgesic activity. Results: All the synthesized 4-(4-fluoro-3-methylphenyl)-6-(substituted aryl)-1,6-dihydro pyrimidin-2-ol derivatives were characterized by Fourier-transform infrared spectroscopy,1H nuclear magnetic resonance, mass spectroscopy, and bases of elemental analysis. The result of biological screening revealed that many of the new derivatives were endowed with improved anti-inflammatory and analgesic activities. Conclusion: Nature of the substituent played a major role in anti-inflammatory and analgesic activities. The pyrimidine derivative with chlorophenyl substitution exhibited potent anti-inflammatory and analgesic activities. From the results, it was concluded that 6-(4-chlorophenyl)-4-(4-fluoro-3- methyl phenyl)-1,6-dihydropyrimidin-2-ol was the most active compound.

Design and Synthesis of Quinazolinone Derivatives as Anti-inflammatory Agents: Pharmacophore Modeling and 3D QSAR Studies

2014 ◽  
Vol 10 (7) ◽  
pp. 711-723 ◽  
Author(s):  
P. Chaitanya ◽  
G. Reddy ◽  
G. Varun ◽  
L.M. Srikanth ◽  
V.V.S.R. Prasad ◽  
...  
Keyword(s):  
3D Qsar ◽  
Pharmacophore Modeling ◽  
Qsar Studies ◽  
Design And Synthesis ◽  
Anti Inflammatory ◽  
Quinazolinone Derivatives

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 and analgesic effects of methanol extract of red cultivar Allium cepa bulbs in rats and mice

2021 ◽  
Vol 0 (0) ◽  
Author(s):  
Adeoye Joshua Oyewusi ◽  
Olayinka Ayotunde Oridupa ◽  
Adebowale Bernard Saba ◽  
Ibironke Kofoworola Oyewusi ◽  
Jonny Olufemi Olukunle
Keyword(s):  
Allium Cepa ◽  
Methanol Extract ◽  
Biological Activities ◽  
Hot Water ◽  
Control Group ◽  
Tail Flick ◽  
Control Groups ◽  
Inflammatory Models ◽  
Paw Oedema ◽  
Anti Inflammatory

Abstract Objectives Several cultivars of Allium cepa L. have been studied for anti-inflammatory and analgesic activities but there is inadequate information on such biological activities of the concentrated extracts of the Nigerian grown red cultivar A. cepa bulb. Methods The anti-inflammatory models used in this study were Carrageenan-induced paw oedema and formalin-induced paw lick in rats, while acetic acid-induced abdominal writhing, hot plate reaction, hot water tail flick tests in mice were the analgesic models. Results At 30 min post-induction (pi), the inhibition of paw oedema (62.50%) by 200 mg/kg of methanol extract of red cultivar A. cepa bulb (MERCACB) was significantly (p<0.001) higher than that of indomethacin (15.63%) at 10 mg/kg. The paw oedema inhibition at 60 min pi by MERCACB (76.92%) was significantly higher than that of indomethacin (41.03%). At the early phase of formalin paw-lick test, the pain reaction time (PRT) of rat treated with MERCACB (400 mg/kg) was significantly lower than that of indomethacin and the control groups. The hotplate test revealed that PRT of mice treated with 800 mg/kg of MERCACB were significantly (p<0.01) longer in comparism to indomethacin and control groups. The PRT of mice subjected to thermal pain due to hot water and treated with 800 mg/kg of MERCACB was significantly (p<0.05) longer than that of the control group. Conclusions These findings indicate that MERCACB possesses potent anti-inflammatory and analgesic properties which confirm the traditional use of the plant for the treatment of inflammatory diseases and may be useful as a future therapeutic agent.

Synthesis, characterization, and evaluation of some novel 4(3H)-quinazolinone derivatives as anti-inflammatory and analgesic agents

2012 ◽  
Vol 22 (1) ◽  
pp. 440-452 ◽  
Author(s):  
Awatef A. Farag ◽  
Ebtsam M. Khalifa ◽  
Naima A. Sadik ◽  
Samir Y. Abbas ◽  
Abdullah G. Al-Sehemi ◽  
...  
Keyword(s):  
Analgesic Agents ◽  
Anti Inflammatory ◽  
Quinazolinone Derivatives

scholarly journals Preliminary assessment of the anti-inflammatory and analgesic effects of methanol leaf extract of Cussonia barteri (Araliaceae) in rodents

2019 ◽  
Vol 65 (3) ◽  
pp. 22-31
Author(s):  
Ighodaro Igbe ◽  
Osaze Edosuyi ◽  
Agbonlahor Okhuarobo ◽  
Adarki Pongri ◽  
Nkechi Maduako ◽  
...  
Keyword(s):  
Acetic Acid ◽  
Analgesic Effect ◽  
Leaf Extract ◽  
Methanol Extract ◽  
Tail Flick ◽  
Hot Plate ◽  
Analgesic Effects ◽  
Paw Oedema ◽  
Anti Inflammatory ◽  
Ear Oedema

Summary Introduction: Potato (Solanum tuberosum L.) is an important vegetable crop in Syria. Potato tuber moth Cussonia barteri is a small tree that grows in the sub-Saharan part of Africa. Various parts of the plant are used for the treatment of a variety of ailments in ethno-medicine. Objective: To evaluate the anti-inflammatory and analgesic effect of the methanol leaf extract of Cussonia barteri. Material and methods: The leaves were air-dried, powdered and repeatedly extracted with methanol using a Soxhlet apparatus. The resulting methanol extract (100, 200 and 400 mg/kg) was evaluated for anti-inflammatory activity using carrageenan-induced paw oedema, xylene-induced ear oedema and formalin-induced arthritis tests. Analgesic effect was evaluated using acetic acid-induced mouse writhing, hot plate and tail flick tests. Results: All doses of the extract significantly (p<0.05) reduced carrageenan-induced paw oedema, however the 400 mg/kg dose gave a sustained effect. The extract significantly inhibited xylene induced ear oedema at all doses. There were no significant (p>0.05) reductions in paw swellings due to formalin. In the acetic acid induced writhing test, the extract significantly (p<0.05) decreased writhing at 400 mg/kg only. Reaction times were not significantly different from the control in the hot plate and tail flick tests. Conclusion: This study has shown that the methanol extract possesses acute anti-inflammatory and peripherally mediated analgesic effects.

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.

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