SYNTHESIS AND EVALUATION OF SOME NOVEL TRIAZOLO BETA-LACTAM DERIVATIVES FOR THEIR ANTI-INFLAMMATORY ACTIVITY

INDIAN DRUGS ◽  
2014 ◽  
Vol 51 (01) ◽  
pp. 48-54
Author(s):  
◽  
N.B Wable ◽  
D.S Musmade ◽  
V. B. Gawali ◽  
J. S. Pattan ◽  
...  
Keyword(s):  
1H Nmr ◽  
Inflammatory Activity ◽  
Beta Lactam ◽  
Standard Drug ◽  
Anti Inflammatory

A series of substituted triazole based β-Lactam derivatives were synthesized. The structures of the synthesized compounds were characterized and confirmed by IR, 1H- NMR and CHN analysis. The synthesized compounds were evaluated for their anti-inflammatory activity. All the compounds have shown promising anti-inflammatory activity when compared with standard drug Ibuprofen.

scholarly journals Synthesis, Characterization and Anti-inflammatory Activity of (2E)-3-(2-Bromo-6-hydroxy-4-methoxyphenyl)-1-(naphthalene-2-yl)prop-2-en-1-one

2020 ◽  
Vol 32 (3) ◽  
pp. 561-564
Author(s):  
Dileep Kumar M. Guruswamy ◽  
Shankar Jayarama
Keyword(s):  
1H Nmr ◽  
13C Nmr ◽  
Stair Climbing ◽  
Inflammatory Activity ◽  
Spectral Studies ◽  
Albino Rats ◽  
Paw Edema ◽  
Standard Drug ◽  
Edema Model ◽  
Anti Inflammatory

(2E)-3-(2-Bromo-6-hydroxy-4-methoxyphenyl)-1-(naphthalene-2-yl)prop-2-en-1-one (d1) was synthesized by the Claisen-Schmidt condensation method and characterized by 1H NMR, 13C NMR spectral studies. The anti-inflammatory activity was conducted in Swiss albino rats for paw edema model. Edema was actuated with 1 % carrageenan to every one of the animals following 1 h of the oral medicines. Paw thickness was checked at t = 1, 2, 3, 4, 5 and 24 h. Stair climbing score and motility score were surveyed at t = 24 h. Compound d1 signicant decline in paw thickness at p < 0.001 diminished by 32 % in paw thickness. The compound d1 signicantly expanded the stair climbing and motility score. This study suggested that the compound d1 exhibits remarkable anti-inflammatory activity when compared with that of the standard drug.

Design, Synthesis, Characterization and in silico molecular docking studies and in vivo anti-inflammatory Activity of Pyrazoline clubbed Thiazolinone Derivatives

2020 ◽  
Vol 17 ◽  
Author(s):  
Deepak Kumar Singh ◽  
Mayank Kulshreshtha ◽  
Yogesh Kumar ◽  
Pooja A Chawla ◽  
Akash Ved ◽  
...  
Keyword(s):  
Molecular Docking ◽  
Biological Activities ◽  
Inflammatory Activity ◽  
Standard Drug ◽  
Docking Score ◽  
Chemical Structures ◽  
Cox 2 ◽  
Anti Inflammatory ◽  
Cox 1

Background: The pyrazolines give the reactions of aliphatic derivatives, resembling unsaturated compounds in their behavior towards permanganate and nascent hydrogen. This nucleus has been associated with various biological activities including inflammatory. Thiazolinone is a heterocyclic compound that contains both sulfur and nitrogen atom with a carbonyl group in their structure.Thiazolinone and their derivatives have attracted continuing interest because of their various biological activities, such as anti-inflammatory, antimicrobial, anti-proliferative, antiviral, anticonvulsant etc. The aim of the research was to club pyrazoline nucleus with thiazolinone in order to have significantanti-inflammatory activity. The synthesized compounds were chemically characterized for the establishment of their chemical structures and to evaluate as anti-inflammatory agent. Method: In the present work, eight derivatives of substituted pyrazoline (PT1-PT8) were synthesized by a three step reaction.The compounds were subjected to spectral analysis by Infrared, Mass and Nuclear magnetic resonance spectroscopy and elemental analysis data. All the synthesized were evaluated for their in vivo anti-inflammatory activity. The synthesized derivatives were evaluated for their affinity towards target COX-1 and COX-2, using indomethacin as the reference compound molecular docking visualization through AutoDock Vina. Results: Compounds PT-1, PT-3, PT-4 and PT-8 exhibited significant anti-inflammatory activity at 3rd hour being 50.7%, 54.3%, 52.3% and 57% respectively closer to that of the standard drug indomethacin (61.9%).From selected anti-inflammatory targets, the synthesized derivatives exhibited better interaction with COX-1 and COX-2 receptor, where indomethacin showed docking score of -6.5 kJ/mol, compound PT-1 exhibited highest docking score of -9.1 kJ/mol for COX-1 and compound PT-8 having docking score of 9.4 kJ/mol for COX-2. Conclusion: It was concluded that synthesized derivatives have more interaction with COX-2 receptors in comparison to the COX-1 receptors because the docking score with COX-2 receptors were very good. It is concluded that the synthesized derivatives (PT-1 to PT-8) are potent COX-2 inhibitors.

A Facile One-Pot Synthesis of 3-Methylbenzisoxazoles via a Key Intermediate of ortho-Ethoxyvinyl Nitroaryls by Domino Rearrangement and Their Anti- Inflammatory Activity

2020 ◽  
Vol 16 (8) ◽  
pp. 1161-1165
Author(s):  
Bashetti Nagaraju ◽  
Jagarlapudi V. Shanmukhakumar ◽  
Nareshvarma Seelam ◽  
Tondepu Subbaiah ◽  
Bethanamudi Prasanna
Keyword(s):  
Stannous Chloride ◽  
Biologically Active ◽  
Inflammatory Activity ◽  
Albino Rats ◽  
One Pot ◽  
Simple Method ◽  
Standard Drug ◽  
Entire Study ◽  
One Pot Synthesis ◽  
Anti Inflammatory

Background: Recently, there has been a lot of scientific interest in exploring the syntheses of oxygen and nitrogen-containing heterocyclic compounds due to their pharmacological activities. In addition, benzisoxazoles play a very important role in organic synthesis as key intermediates. Objective: In this paper, we focused on developing a novel synthetic route for biologically active arylisoxazoles under normal conditions, and simplified it to get high purities and yields, and also reported their anti-inflammatory activities. Method: An efficient and simple method has been explored for the synthesis of novel 3-methyl arylisoxazoles from o-nitroaryl halides via o-ethoxyvinylnitroaryls, using dihydrated stannous chloride (SnCl2.2H2O) in MeOH / EtOAc (1:1) via Domino rearrangement in one pot synthesis. Result: We synthesized novel 3-methylarylisoxazoles from o-nitroarylhalides via o-ethoxyvinylnitroaryls, using dihydrated stannous chloride (SnCl2.2H2O) in MeOH / EtOAc (1:1) via domino rearrangement. In this reduction, nitro group and ethoxy vinyl group change to the functional acyl ketones, followed by hetero cyclization. Here, the reaction proceeds without the isolation of intermediates like 2-acylnitroarenes and 2- acylanilines. All the synthesized compounds were completely characterized by the NMR and mass spectra. The compounds were also explored for their anti-inflammatory activity by carrageenan-induced inflammation in the albino rats (150-200 g) of either sex used in this entire study with the use of Diclofenac sodium as the standard drug. The initial evaluations identified leading targets with good to moderate anti-inflammatory activity. Conclusion: A simple, one-pot and convenient method has been explored for the synthesis of novel 3- methylarylisoxazoles with high purity and reaction yields. All the compounds 3a, 3c, 3d, 3f, 3g and 3h exhibited 51-64% anti-inflammatory activities.

Design and Synthesis of Novel Anti-inflammatory/Anti-ulcer Hybrid Molecules with Antioxidant Activity

2020 ◽  
Vol 16 ◽  
Author(s):  
Bhim Bahadur Chaudhari ◽  
Alka Bali ◽  
Ajitesh Balaini
Keyword(s):  
Antioxidant Activity ◽  
Oral Absorption ◽  
Radical Scavenging ◽  
Reducing Power ◽  
Antioxidant Potential ◽  
Inflammatory Activity ◽  
In Vivo Models ◽  
Standard Drug ◽  
Hybrid Molecules ◽  
Anti Inflammatory

Background: NSAIDs are the most widely prescribed medications worldwide for their anti-inflammatory, antipyretic, and analgesic effects However, their chronic use can lead to several adverse drug events including GI toxicity. The selective COX-2 inhibitors developed as gastro-sparing NSAIDs also suffer from serious adverse effects which limit their efficacy. Objective: Local generation of reactive oxygen species is implicated in NSAID-mediated gastric ulceration and their combination with H2 antagonists like famotidine reduces the risk of ulcers. The objective of this work was to design and synthesize novel methanesulphonamido isoxazole derivatives by hybridizing the structural features of NSAIDs with those of antiulcer drugs (ranitidine, famotidine, etc.) to utilize a dual combination of anti-inflammatory activity and reducing (antioxidant) potential. Method: The designing process utilized three dimensional similarity studies and utilized an isoxazole core having a potential for anti-inflammatory as well as radical scavenging antioxidant activity. The compounds were assayed for their antiinflammatory activity in established in vivo models. The in vitro antioxidant activity was assessed in potassium ferricyanide reducing power (PFRAP) assay employing ascorbic acid as the standard drug. Results: Compounds (5, 6, 9 and 10) showed anti-inflammatory activity comparable to the standard drugs and were also found to be non-ulcerogenic at the test doses. Compounds 6-10 exhibited good antioxidant effect in the concentration range of 1.0-50.0 µmol/ml. The test compounds were also found to comply with the Lipinski rule suggesting good oral absorption. Conclusion: A new series of isoxazole based compounds is being reported with good anti-inflammatory activity coupled with antioxidant potential as gastro-sparing anti-inflammatory agents.

scholarly journals Synthesis, Characterization and Evaluation of Anti-inflammatory Activity of Novel Indoline Derivatives

2016 ◽  
Vol 12 (12) ◽  
pp. 4557-4563
Author(s):  
Dhinesh kumar Manoharan
Keyword(s):  
1H Nmr ◽  
13C Nmr ◽  
Protein Denaturation ◽  
Inflammatory Activity ◽  
Potent Inhibition ◽  
Ft Ir ◽  
Anti Inflammatory

Series of indoline derivatives were synthesized using N-(4-aminophenyl) indoline-1-carbothiamide as a precursor. The structures of synthesized compounds were confirmed by   FT-IR, 1H-NMR, 13C-NMR and LC-MS. The in vitro anti-inflammatory activity of synthesized indoline derivatives were examined by standard anti-denaturation assay. The compounds 4a (IC50 = 62.2 µg/ml) and 4b (IC50 = 60.7 µg/ml) showed potent inhibition on protein denaturation. The compounds 5a (IC50 = 97.8 µg/ml) exhibits moderate inhibition on protein denaturation

scholarly journals Anti-Inflammatory Activity of Chrozophora rottleri Extracts on Carrageenan-Induced Rat Paw Edema

2016 ◽  
Vol 3 ◽  
pp. 20-26
Author(s):  
Mallikarjuna Rao Talluri ◽  
Battu Ganga Rao ◽  
Y. Venkateswaea Rao
Keyword(s):  
Ethyl Acetate ◽  
Methanol Extract ◽  
Bioactive Molecules ◽  
Inflammatory Activity ◽  
Paw Edema ◽  
Standard Drug ◽  
Isolation And Characterization ◽  
Rat Paw Edema ◽  
Anti Inflammatory ◽  
Rat Paw

The present study was intended to evaluate Anti-inflammatory activity ofC. rottleriextracts (Hydroalcoholic, Methanol, Ethyl acetate and Hexane). The Anti-inflammatory activity ofC.rottleriextracts at doses of 125mg/kg, 250mg/kg and 500mg/kg using carrageenan induced rat paw edema model compared with standard drug (Indomethacin). The selected plant extracts significantly inhibited paw edema along with the standard drug Indomethacin. Of all extracts, methanol extract produced significant effect on reduction of increased paw thickness, hydro alcoholic and ethyl acetate extracts produced moderate percentage inhibition and hexane extract produced low level of percentage inhibition in reducing paw edema on carrageenan induced rats. In all extracts, methanol extract at a dose of 500mg/kg showed more percentage inhibition i.e . 53.47±2.19. From the results obtained during the study it is concluded thatC. rottlerihaving the bioactive molecule responsible for Anti-inflammatory activity by individually or by combination of different bio-active compounds present in it. Further is necessary for isolation and characterization of bioactive molecules which are responsible for the selected plant biological activities.

scholarly journals ANTI-INFLAMMATORY ACTIVITY OF NIGELLA SATIVA SILVER NANOPARTICLES: BIOCHEMICAL STUDY

2019 ◽  
pp. 346-349
Author(s):  
GOMATHI KANNAYIRAM ◽  
SANDHYA A ◽  
SOWMIYA S ◽  
VALARMATHI S ◽  
DANIEL JOSEPH
Keyword(s):  
Silver Nanoparticles ◽  
Protein Denaturation ◽  
Nigella Sativa ◽  
Inflammatory Activity ◽  
Assay Method ◽  
Enzyme Linked Immunosorbent Assay ◽  
Infrared Analysis ◽  
Standard Drug ◽  
Rbc Membrane ◽  
Anti Inflammatory

Objective: The aim of this study is to evaluate the anti-inflammatory activity of Nigella sativa silver nanoparticles (NS AgNPs). Methods: Fourier transform infrared analysis was used to characterize the NS AgNPs and the extract. 2,2-diphenylpicrylhydrazyl assay was done to test the antioxidant potency of NS AgNP. Furthermore, in vitro anti-inflammatory activity of the extract and the NS AgNP was determined by red blood cell (RBC) membrane stabilization assay, protein inhibition assay, and interleukin-1 (IL-1) beta assay. Results: The NS AgNP exhibited dose-dependent antioxidant property. At the concentration 0.01 mg/ml 80% of radical was scavenged by NS AgNP. Inhibition of protein denaturation assay also suggests that NS AgNP shows the highest activity (70%) when compared with the standard drug aspirin (65%). RBC assay suggests that NS AgNP stabilizes the RBC membrane and prevents leaking. In the enzyme-linked immunosorbent assay method the NS AgNP showed better IL-1 beta inhibition activity when compared to aqueous extract. Conclusion: From the study, it was inferred that NS AgNPs are more effective when compared to the extract. These results suggest that NS AgNP can be used to treat inflammatory disorders.

scholarly journals Anti-Inflammatory Activity of Hydroxytriazenes and their Vanadium Complexes

2008 ◽  
Vol 5 (s2) ◽  
pp. 1144-1148 ◽  
Author(s):  
Kalpana Singh ◽  
Peeyush Patel ◽  
A. K. Goswami
Keyword(s):  
Body Weight ◽  
Metal Complexes ◽  
Diclofenac Sodium ◽  
Inflammatory Activity ◽  
Albino Rats ◽  
Vanadium Complexes ◽  
Standard Drug ◽  
Standard Methods ◽  
Paw Oedema ◽  
Anti Inflammatory

The anti-inflammatory activity of hydroxytriazenes as well as their vanadium complexes has been studied using carrageenan induced hind paw oedema method in albino rats (Wister strain). Hydroxytriazenesviz., 3-hydroxy-1,3-diphenyltriazene(HT-1), 3-hydroxy-3-phenyl-1-(4-sulfonamido)phenyl triazene(HT-2), 3-hydroxy-3-p-chlorophenyl-1-(4-sulfonamido) phenyltriazene(HT-3), 3-hydroxy-3-m-chlorophenyl-1-(4-sulfonamido)phenyltriazene(HT-4)(HT-4) and their respective vanadium complexes C-1, C-2, C-3 and C-4 have been synthesized using standard methods, purified, characterized and used for studying their anti-inflammatory activities. The hind paw oedema was produced by subplanter injection of carrageenan and the paw volume was measured plethysmographically after 0.5, 1, 2, 3 and 5 h. The animals were givenHT-1, HT-2, HT-3andHT-4and also vanadium complexes C-1, C-2, C-3 and C-4 dissolved inDMSO(at dose 5 mg/Kg body weight). Diclofenac sodium (5 mg/kg) was used as a standard drug. The standard drug shows maximum inibition up to 1h as 81.73% which goes on increasing up to 3h (88.94%) but further reduces to 74.93% at the end of 5 h. The test compounds i.e. both ligands as well as their metal complexes show maximum percent inhibition only up to 1h. after which the efficacy reduces. Thus it can be said that both ligands as well as their vanadium complexes show very significant anti-inflammatory activity up to 1h which is comparable to standard drug.

scholarly journals Methanolic Extract of Leathery Murdah, Terminalia coriacea (Roxb.) Wight and Arn. Leaves Exhibits Anti-Inflammatory Activity in Acute and Chronic Models

2018 ◽  
Vol 27 (3) ◽  
pp. 267-271 ◽  
Author(s):  
Mohammed Safwan Ali Khan ◽  
Nishath Khatoon ◽  
Mohammad M. Al-Sanea ◽  
Mohamed Gamal Mahmoud ◽  
Hidayat Ur Rahman
Keyword(s):  
Methanolic Extract ◽  
Test Dose ◽  
Inflammatory Activity ◽  
Paw Edema ◽  
Standard Drug ◽  
Inflammatory Models ◽  
Cotton Pellet ◽  
Wet Weight ◽  
Granulomatous Tissue ◽  
Anti Inflammatory

Objective: The aim of the present study was to evaluate anti-inflammatory activity of methanolic extract of Terminalia coriacea. Materials and Methods: A methanolic extract of T. coriacea leaves was studied in albino Wistar rats with carrageenan-induced paw edema, an acute model, and cotton pellet-induced granuloma, a chronic model, at 3 oral test doses (125, 250, and 500 mg/kg). Aspirin 100 mg/kg was used as a positive control. Paw volume and wet and dry weights of cotton pellets were determined. The data were analyzed by one-way ANOVA followed by Dunnett’s multiple comparison test. Results: The test extract at doses of 125 and 250 mg/kg decreased paw volume and wet and dry weights of cotton pellets. The highest test dose (500 mg/kg) displayed a response comparable to that of the standard drug (p < 0.01) on paw volume. The extract produced similar (p < 0.05) decrease in wet weight of the cotton pellet at 125 and 250 mg/kg, whereas the effect of 500 mg/kg of the extract was comparable to that of aspirin 100 mg/kg (p < 0.01). The extract of T. coriacea at 500 mg/kg induced the most significant (p < 0.01) effect on wet weight of granulomatous tissue. Conclusion: The methanolic extract of T. coriacea leaves successfully decreased paw edema as well as dry and wet weights of granulomatous tissue in both acute and chronic inflammatory models thus confirming the anti- edematogenic, antitransudative, and antiproliferative properties of T. coriacea.

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.

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