Design, Synthesis, Characterization, Anti-Inflammatory and Antioxidant Evaluation of Certain Novel Pyrazoline Derivatives Containing Imidazo[2,1-b]thiazole Moiety

2020 ◽  
Vol 5 (1) ◽  
pp. 45-50
Author(s):  
V.D. Sonawane ◽  
B.D. Sonawane ◽  
M.J. Dhanavade ◽  
K.D. Sonawane ◽  
R.B. Bhosale
Keyword(s):  
Antioxidant Activity ◽  
Antioxidant Activities ◽  
Design Synthesis ◽  
Standard Drug ◽  
Drug Designing ◽  
Antioxidant Evaluation ◽  
Future Drug ◽  
Anti Inflammatory

In present study, a novel series of substituted imidazo[2,1-b]thiazole pyrazoline derivatives (2a-e) and (3a-e) from the reference compound imidazo[2,1-b]thiazole chalcones (1a-e) in PEG-400 by using hydrazine hydrate and phenyl hydrazine was synthesized. Characterization of newly synthesized compounds was done using IR and 1H NMR. Further, imidazo[2,1-b]thiazole pyrazoline derivatives were subjected to check their in vitro antioxidant activities at a concentration of 0.5 mmol/L in methanol. Compounds 2c, 2d, 3c, 3d and 3e showed comparatively good activity than standard drug diclofenac. The anti-inflammatory activity of compounds 2c, 2d, 2e, 3c, 3d and 3e were comparable with standard drug. Similarly, all these compounds possess good antioxidant activity as compared to ascorbic acid (vitamin C); compared to the value of DPPH and SOD antioxidant activity 44.18 % and 74.07 %, respectively. These synthesized compounds exhibited a good anti-inflammatory and antioxidant activities hence might be useful in future drug designing studies.

scholarly journals Design, Synthesis, in Vitro Antioxidant, Anti-Inflammatory and Antidiabetic Evaluation of New N-Substitutedbenzylidene-5-(4-Formylphenyl)-(3-Hydroxyphenyl)-4,5-Dihydropyrazole-1-Carbothioamide Derivatives

2020 ◽  
Author(s):  
Sucheta Singh Singh ◽  
sumit Tehlan Tehlan ◽  
prabhakar kumar verma
Keyword(s):  
Antioxidant Activity ◽  
Heterocyclic Compounds ◽  
Inflammatory Activity ◽  
Antidiabetic Activity ◽  
Design Synthesis ◽  
Standard Drug ◽  
Wide Range ◽  
Anti Inflammatory ◽  
Clinical Potential

Abstract A series of N-substitutedbenzylidene-5-(4-formylphenyl)-(3-hydroxyphenyl)-4,5-dihydropyrazole-1-carbothioamide derivatives was designed, synthesized and examined for their therapeutical potential against prooxidant (oxidative stress), inflammation and diabetes. Biological results showed antioxidant activity with IC50 value 37.68 mol/L, anti-inflammatory activity with IC50 value 26.40 mol/L and antidiabetic activity with IC50 value 17.12 mol/L. The results of antioxidant activity showed that compounds Y9 and Y17 exhibited excellent antioxidant activity with IC50 values 17.43 mol/L and 18.98 mol/L, results of anti-inflammatory activity showed that compounds Y2, Y3 and Y7 exhibited excellent anti-inflammatory activity with IC50 values 23.23 mol/L, 22.09 mol/L and 19.05 mol/L respectively and results of antidiabetic activity showed that compounds Y1, Y5and Y6 exhibited excellent antidiabetic activity with IC50 values 17.08 mol/L, 8.36 mol/L and 13.50 mol/L. When compared with ascorbic acid, aspirin and acarbose as standard drug respectively. Heterocyclic compounds have diversity in their structure which makes them broad and economical therapeutic agents. Pyrazole is a five membered ring containing three carbon and two neighboring nitrogen atoms. Pyrazole and its derivatives have various biological as well as clinical potential thus considered for further research. Due to wide range of therapeutical activities pyrazole makes interest among researcher to explore it further for more activities. Pyrazole is present in various biological moieties eg. antimicrobial, antidiabetic, anti-inflammatory, antioxidant, antiviral, anticonvulsant, anticancer, anti-HIVand anti-tuberculosis agents.

scholarly journals IN VITRO ANTI-INFLAMMATORY AND ANTIOXIDANT ACTIVITIES OF HINGULESWARA RASABASED HERBOMINERAL FORMULATIONS

2018 ◽  
Vol 11 (14) ◽  
pp. 24
Author(s):  
Abhishek Chatterjee ◽  
Dileep Singh Baghel ◽  
Bimlesh Kumar ◽  
Saurabh Singh ◽  
Narendra Kumar Pandey ◽  
...  
Keyword(s):  
Antioxidant Activities ◽  
Radical Scavenging ◽  
Standard Drug ◽  
Three Samples ◽  
Anti Inflammatory ◽  
Dose Dependent ◽  
Antioxidant Effects ◽  
Made In ◽  
In Vitro Antioxidant Activity

Objective: The aims of the present investigation were to develop the herbal and/or herbomineral formulations of Hinguleswara rasa and to compare their anti-inflammatory and antioxidant activities, in vitro, with that of standard drug samples.Methods: This study was an interventional investigation in three samples: In the first sample, Hinguleswara rasa (HR1) was prepared as per methodology described in Rasatarangini using Shuddha Hingula (10 g), Shuddha Vatsanabha (10 g), and Pippali (10 g). In the second and third sample, respectively, Hinguleswara rasa was prepared by replacing Shuddha Hingula with Kajjali where Kajjali made from Hingulotha parada and Sodhita parada constitutes two varieties of Hinguleswara rasa, i.e. HR2 and HR3. In vitro antioxidant activity was studied using 2,2-diphenyl-1-picrylhydrazyl, and the absorbance was recorded at 517 nm. For evaluating the in vitro anti-inflammatory studies, the inhibition of albumin denaturation technique was performed.Results: The results showed that the formulation of Hinguleswara rasa has shown dose-dependent activity which was observed in 100 μg concentration. HR1, HR2, and HR3 showed 36.11, 17.22, and 16.11% radical scavenging activity.Conclusion: It could be concluded that the changes made in the formulations did not affect the in vitro anti-inflammatory and antioxidant effects of the herbomineral formulations.

scholarly journals SYNTHESIS, ANTIOXIDANT AND ANTI-INFLAMMATORY ACTIVITIES OF ETHYL 2-(2-CYANO-3- (SUBSTITUTED PHENYL)ACRYLAMIDO)-4,5-DIMETHYLTHIOPHENE-3-CARBOXYLATES

2017 ◽  
Vol 10 (7) ◽  
pp. 95 ◽  
Author(s):  
Madhavi K ◽  
Sree Ramya G
Keyword(s):  
Antioxidant Activity ◽  
Free Radical ◽  
Antioxidant Properties ◽  
Inflammatory Activity ◽  
Paw Edema ◽  
Standard Drug ◽  
Rat Paw Edema ◽  
Anti Inflammatory ◽  
Rat Paw

Objective: Objective of the study was to synthesize and evaluate a series of novel compounds, ethyl 2-(2-cyano-3-(substituted phenyl)acrylamido)- 4,5-dimethylthiophene-3-carboxylates, for in vitro antioxidant and in vivo anti-inflammatory activities.Methods: Ethyl 2-(2-cyano-3-(substituted phenyl)acrylamido)-4,5-dimethylthiophene-3-carboxylates were synthesized by knoevenagel condensation of active methylene group of ethyl 2-(2-cyanoacetamido)-4,5-dimethylthiophene-3-carboxylate with substituted benzaldehydes. The synthesized compounds were evaluated for their in vitro antioxidant properties in three different models, viz., reduction of 1,1-diphenyl-2-pycrylhydrazyl free radical, scavenging of nitric oxide free radical, and ferric ion-induced lipid peroxidation using rat brain homogenate. Few selected compounds with good antioxidant properties were pharmacologically evaluated for anti-inflammatory activity by carrageenan-induced rat paw edema model.Results: Clean and efficient synthetic procedure was used for the preparation of series of compounds. The structures of synthesized compounds were confirmed by infrared, 1H nuclear magnetic resonance and mass spectra. The antioxidant activity data revealed that the compounds of ethyl 2-(2-cyano-3-(substituted phenyl)acrylamido)-4,5-dimethylthiophene-3-carboxylate containing phenolic substitution showed greater antioxidant activity. Hence, the active compounds were evaluated for anti-inflammatory activity and found to possess good activity. The percentage inhibition of rat paw edema obtained for the evaluated compounds was in the range of 70.2-83.1, comparable to the standard drug diclofenac (85.0%).Conclusion: The use of inexpensive, eco-friendly and readily available reagents, easy work-up and high purity of products makes the procedure a convenient and robust method for the synthesis of title compounds. The compounds of ethyl 2-(2-cyano-3-(substituted phenyl)acrylamido)-4,5- dimethylthiophene-3-carboxylate containing phenolic substitution showed greater antioxidant and anti-inflammatory activities.

scholarly journals Design, Synthesis and Characterization of Some Novel benzamide derivatives and it's Pharmacological Screening

2020 ◽  
pp. 68-74 ◽  
Author(s):  
Akshay R. Yadav ◽  
Shrinivas K. Mohite
Keyword(s):  
Chemical Structure ◽  
Design Synthesis ◽  
Different Types ◽  
Anti Inflammatory ◽  
Benzoyl Isothiocyanate ◽  
Pharmacological Screening ◽  
Benzamide Derivatives

The new series of substituted N-(phenylcarbamothioyl)benzamide derivatives (2a-2f) was designed, development and synthesized by using conventional and microwave method. In present work 6 different N-(phenylcarbamothioyl)benzamide were synthesized. Substituted benzoyl chloride is converted into benzoyl isothiocyanate by esterification. Benzoyl isothiocyanate is converted into Substituted (phenylcarbamothioyl)benzamide by treating with different types of substituted aniline. Confirmation of the chemical structure of the synthesized was substantiated by TLC, IR, 1H NMR, MS spectroscopy.Novel synthesized compounds screened for their in vivo and in-vitro anti-inflammatory studies and compound 2f shows promising anti-inflammatory activity.

scholarly journals Phenolic Content, Antioxidant Activity, Anti-Inflammatory Potential, and Acute Toxicity Study of Thymus leptobotrys Murb. Extracts

2020 ◽  
Vol 2020 ◽  
pp. 1-7
Author(s):  
Asmaa Oubihi ◽  
Hanae Hosni ◽  
Issmail Nounah ◽  
Abdessamad Ettouil ◽  
Hicham Harhar ◽  
...  
Keyword(s):  
Antioxidant Activity ◽  
Female Rats ◽  
Trolox Equivalent Antioxidant Capacity ◽  
Control Group ◽  
Standard Drug ◽  
Methanolic Extracts ◽  
Anti Inflammatory ◽  
Inflammatory Effect

Thymus leptobotrys is a medicinal plant belonging to the Lamiaceae family, endemic in Morocco, and used in traditional medicine. The present work aims to study the phenolic compounds, the antioxidant activity, the anti-inflammatory effect, and the toxicity of two ethanolic and methanolic extracts of Thymus leptobotrys aerial part. The yield of the methanolic extraction (22.2%) is higher than that of the ethanolic extraction (15.8%) and is characterized by higher contents of polyphenols 243.08 mg/g GAE (mg/g of gallic acid), flavonoids 179.28 mg/g RE (mg/g of rutin), and tannins 39.31 mg/g CE (mg/g of catechin). The in vitro measurement of antioxidant activity with the 2,2-diphenyl-1-picrylhydrazyl (DPPH) radical reduction test and Trolox equivalent antioxidant capacity (TEAC) test demonstrates the higher performance of the methanolic extract. The evaluation of the anti-inflammatory effect in vivo on adult Wistar female rats leads to a very significant decrease in the inflammation of the edema compared to the standard drug (indomethacin) and the control group. The toxicity test reveals that both extracts showed no toxicity within an LD50 above 2000 mg/kg body weight of the rats.

scholarly journals Design and Synthesis of π-Extended Resveratrol Analogues and In Vitro Antioxidant and Anti-Inflammatory Activity Evaluation

Molecules ◽  
2021 ◽  
Vol 26 (3) ◽  
pp. 646
Author(s):  
Ki Yoon Nam ◽  
Kongara Damodar ◽  
Yeontaek Lee ◽  
Lee Seul Park ◽  
Ji Geun Gim ◽  
...  
Keyword(s):  
Antioxidant Activity ◽  
Antioxidant Activities ◽  
Biological Effects ◽  
Drug Candidates ◽  
Design And Synthesis ◽  
Study Results ◽  
Resveratrol Analogues ◽  
Anti Inflammatory ◽  
Nitrogen Substitution

The research on resveratrol (1) has been conducted intensively over a long time due to its proven antioxidant activity and disease-fighting capabilities. Many efforts have also been made to increase these biological effects. In the present study, six new extended aromatic resveratrol analogues containing naphthalene (2) and its bioisosteres quinoline (3 and 4), isoquinoline (5) quinoxaline (6) and quinazoline (7) scaffolds were designed and synthesized using an annulation strategy. The antioxidant and anti-inflammatory activities of these compounds were investigated. All compounds showed better antioxidant activity than resveratrol in ABTS assay. As for the anti-inflammatory test, 5 and 7 exhibited better activity than resveratrol. It is worth noting that nitrogen substitution on the extended aromatic resveratrol analogues has a significant impact on cell viability. Taking the antioxidant activities and NO inhibition activities into consideration, we conclude that isoquinoline analogue 5 may qualify for the further investigation of antioxidant and anti-inflammatory therapy. Furthermore, our study results suggest that in order to improve the biological activity of polyphenolic compounds, extended aromaticity and nitrogen substitution strategy could be a viable method for the design of future drug candidates.

scholarly journals Semipurified Ethyl Acetate Partition of Methanolic Extract ofMelastoma malabathricumLeaves Exerts Gastroprotective Activity Partly via Its Antioxidant-Antisecretory-Anti-Inflammatory Action and Synergistic Action of Several Flavonoid-Based Compounds

2017 ◽  
Vol 2017 ◽  
pp. 1-14 ◽  
Author(s):  
Noor Wahida Ismail Suhaimy ◽  
Ahmad Khusairi Noor Azmi ◽  
Norhafizah Mohtarrudin ◽  
Maizatul Hasyima Omar ◽  
Siti Farah Md. Tohid ◽  
...  
Keyword(s):  
Antioxidant Activity ◽  
Ethyl Acetate ◽  
Methanolic Extract ◽  
Antioxidant Activities ◽  
Gastric Wall ◽  
Synergistic Action ◽  
Gastroprotective Activity ◽  
Gastric Mucus ◽  
Anti Inflammatory

Recent study has demonstrated the gastroprotective activity of crude methanolic extract ofM. malabathricumleaves. The present study evaluated the gastroprotective potential of semipurified extracts (partitions): petroleum ether, ethyl acetate (EAMM), and aqueous obtained from the methanolic extract followed by the elucidation of the gastroprotective mechanisms of the most effective partition. Using the ethanol-induced gastric ulcer assay, all partitions exerted significant gastroprotection, with EAMM being the most effective partition. EAMM significantly (i) reduced the volume and acidity (free and total) while increasing the pH of gastric juice and enhanced the gastric wall mucus secretion when assessed using the pylorus ligation assay, (ii) increased the enzymatic and nonenzymatic antioxidant activity of the stomach tissue, (iii) lost its gastroprotective activity following pretreatment with N-omega-nitro-L-arginine methyl ester (L-NAME; NO blocker) or carbenoxolone (CBXN; NP-SH blocker), (iv) exerted antioxidant activity against various in vitro oxidation assays, and (v) showed moderate in vitro anti-inflammatory activity via the LOX-modulated pathway. In conclusion, EAMM exerts a remarkable NO/NP-SH-dependent gastroprotective effect that is attributed to its antisecretory and antioxidant activities, ability to stimulate the gastric mucus production and endogenous antioxidant system, and synergistic action of several gastroprotective-induced flavonoids.

Anti-inflammatory, Analgesic and Antioxidant Activities of the Hydroalcoholic Extract from Celery (Apium graveolens) Leaves

2018 ◽  
Vol 16 (S1) ◽  
pp. S237-S244
Author(s):  
A. Dellal ◽  
F. Toumi-Benali ◽  
M.M. Dif ◽  
S. Bouazza ◽  
S. Brikhou ◽  
...  
Keyword(s):  
Acetic Acid ◽  
Analgesic Activity ◽  
Antioxidant Activities ◽  
Apium Graveolens ◽  
Control Group ◽  
Albino Rats ◽  
Standard Drug ◽  
Hydroalcoholic Extract ◽  
Anti Inflammatory

Celery (Apium graveolensL.) belongs to the Apiaceae family. It is a genus of an annual or biannual herb.A. graveolensis used in Algeria as a medicinal plant for the treatment of many diseases. This study was carried out to assess and confirm the in vivo anti-inflammatory and analgesic effect of hydroalcoholic extract fromA. graveolensleaves. Wistar albino rats of both sexes, with different ages 2–3 months weighing between 160 and 250 g and Swiss albinosmice weighing 22–27 g were used for this study. The antiinflammatory activity was estimated by measuring the oedema induced by Carrageenan; the analgesic activity was performed by the acetic acid–induced writhing test and formalin-induced paw licking. The administration of hydroalcoholic extract at doses of 200, 300 and 500 mg/kg body weight significantly reduced the increase of the paw volume with an inhibition percentage of 80.17%, 86.50% and 89.66%, respectively; all doses showed a strong significant effect (p< 0.001). These results were similar to those obtained with piroxicam 78.93% and indometacine 76.13%. Although the same doses showed a high significant effect (p< 0.01) compared to the control group, the extract at a dose of 500 mg/kg registered higher levels of analgesic activity (17 ± 2.36) writhing (75.53% inhibition) than the standard drug paracetamol (30.5 ± 3.61) writhing; in the two tests, acetic acid induced writhing and formalin induced paw licking. The study of hydroalcoholic extract in vitro showed a high antioxidant capacity by inhibition of 2,2-diphenyl-1-picrylhydrazyl radical (IC50= 1.29 mg/ml). In conclusion,A. graveolensis an interesting plant and the hydroalcoholic leaves extracts could be used scientifically in the treatment of acute inflammation and the peripheral analgesic activity.

scholarly journals Chemical Composition and Antioxidant, Analgesic, and Anti-Inflammatory Effects of Methanolic Extract ofEuphorbia retusain Mice

2018 ◽  
Vol 2018 ◽  
pp. 1-11 ◽  
Author(s):  
Jazia Sdayria ◽  
Ilhem Rjeibi ◽  
Anouar Feriani ◽  
Sana Ncib ◽  
Wided Bouguerra ◽  
...  
Keyword(s):  
Acetic Acid ◽  
Methanolic Extract ◽  
Antioxidant Activities ◽  
Significant Inhibition ◽  
Paw Edema ◽  
Alternative Source ◽  
Standard Drug ◽  
Methanolic Extracts ◽  
Anti Inflammatory

Plants provide an alternative source to manage different human disorders due to various metabolites. The aim of this study is to investigate the phytochemical constituents of the methanolic extracts ofEuphorbia retusaand to evaluate their antioxidant, anti-inflammatory, and analgesic activities. The phytochemical results obtained by HPLC and by chemical assay reactions have revealed the richness of the methanolic extract ofE. retusain active compounds, in particular polyphenols, flavonoids, and tannins. The methanolic extract shows significant antioxidant activitiesin vitro, in the DPPH and the FRAP assays. The antinociceptive activity was evaluated using acetic acid and hot-plate models of pain in mice. The anti-inflammatory activity was evaluated by carrageenan-induced paw edema. Oral pretreatment with the methanolic extract ofE. retusa(200 mg/kg) exhibited a significant inhibition of pain induced either by acetic acid or by the heating plate and in a manner comparable to the standard drug paracetamol.E. retusasignificantly reduced paw edema starting from the 3rd hour after carrageenan administration by increasing the activity of antioxidant enzymes (SOD, CAT, and GPx) in liver and paw tissues and decreasing the levels of MDA. These results may confirm the interesting potential of this plant as a treatment of various inflammatory and pain diseases.

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