scholarly journals Preparation and Characterization of New 1,3,5-Trisubstituted-2-Pyrazolines Derivative for their Anti-Inflammatory Activity

2021 ◽  
pp. 992-1004
Author(s):  
Jitendra Kumar Chaudhary ◽  
Alok Pal Jain ◽  
O. P. Tiwari
Keyword(s):  
Inflammatory Activity ◽  
Paw Edema ◽  
Mass Spectral Analysis ◽  
Phenyl Hydrazine ◽  
Design Synthesis ◽  
Standard Drug ◽  
Mass Spectral ◽  
Anti Inflammatory ◽  
Relevant Degree

The objective of the paper was to design, synthesis and characterization of new 1,3,5-trisubstituted-2-pyrazolines derivative and evaluate for anti-inflammatory potential. The 1,3,5-tri-substituted-2-pyrazolines derivatives has been synthesized by the reaction of chalcone     derivatives with 4-hydrazinylbenzene sulfonamide hydrochloride and phenyl hydrazine hydrochloride. Total Sixteen compounds has been synthesized and characterized by the IR, 1HNMR and mass spectral analysis. Proposed compounds have been evaluated for anti-inflammatory activity. Anti-inflammatory activity of the compounds carried out by two animal     model i.e. Carrageenan induced, paw edema in rats and Inhibition of formalin induced paw edema in rats. Anti-inflammatory activity of the compounds C7, C8 and C2 were shown 98.26,  92.77 and 96.24 percentages of inhibition and compounds D7, D8 and D2  were shown 81.50, 83.81 and 78.32 percentages of inhibition as compared to the standard drug Diclofenac at 10 mg/kg was inhibit the inflammation 99.42 % after 6h. These result is a evident that synthesized compounds show relevant degree of anti-inflammatory activity as compared to the standard drug. It is also concluded that the presence of SO2NH2 group, Cl, CH3, OCH3 and N(CH3)2 group may provide the active compounds when attached to the pyrazoline group. But the addition of OH, Br and no substitution in phenyl ring may diminish the activity. 

scholarly journals DESIGN, SYNTHESIS, AND EVALUATION OF NEW DERIVATIVE OF 1,2,4-TRIAZOLES FOR ANTIMICROBIAL AND ANTI-INFLAMMATORY ACTIVITY

2018 ◽  
Vol 10 (4) ◽  
pp. 29 ◽  
Author(s):  
Prabhu C. Jalihal ◽  
Vaibhav Rajoriya ◽  
Varsha Kashaw
Keyword(s):  
Biological Evaluation ◽  
Study Data ◽  
Inflammatory Activity ◽  
Basic Medium ◽  
Paw Edema ◽  
Zone Of Inhibition ◽  
Design Synthesis ◽  
Standard Drug ◽  
Rat Paw Edema ◽  
Anti Inflammatory

Objective: The object of the study is to design, synthesize and biological evaluation of isoniazid derived 1,2,4-triazoles compounds.Methods: Isoniazid based 1,2,4-triazoles derivatives have been synthesized by reaction of Isoniazid with carbon disulfide in basic medium (KOH) to form Potassium dithiocarbazinate salt and reaction with hydrazine hydrate converted into 4-amino-5-(pyridin-4-yl)-4H-1,2,4-triazole-3-thiol. These compounds were reacted with seven different benzaldehyde to form 4-[(substituted phenyl)-methylene]-amino-5-(pyridine-4-yl)-4H-1,2,4-triazol-3-thiol (4). The final compounds were synthesized by reaction with four different acetanilide to form 4-[substituted phenyl)-methylene]-amino-3-(N-substitutedcarboxamidomethylthio)-5-(pyridine-4-yl)-4H-1,2,4-triazoles derivatives. All these compounds were characterized by IR, 1H-NMR, [13]C-NMR and elemental analysis. The antimicrobial activity was determined by the cup plate method. Acute anti-inflammatory activity determined by using carrageenan-induced rat paw edema model.Results: Series PJ-A4, PJ-A7 and PJ-A13 showed more than 90% of the zone of inhibition against both Gram positive and Gram negative organisms. The antifungal study suggested that among synthesized compounds series PJ-A4, A7, A9, A11 and A13 showed more than 90% of zone of inhibition, A2, A10 and A12 shows more than 80% of the zone of inhibition. Anti-inflammatory study data indicate that compounds PJ-A4, PJ-A8, PJ-A9 and PJ-A13 produced 70 to 76% of paw edema inhibition compare to standard drug Ibuprofen which showed 83.3% after 5 h. Conclusion: Results suggested that the isoniazid based 1,2,4-triazole derivatives have significant antibacterial, antifungal and anti-inflammatory activity.

scholarly journals Synthesis and Anti-Inflammatory Activity of a Novel Series of Diphenyl-1,2,4-triazoles and Related Derivatives

2012 ◽  
Vol 9 (4) ◽  
pp. 2510-2515 ◽  
Author(s):  
Swapna Cherala ◽  
Harikiran Lingabathula ◽  
Rama Ganta ◽  
Srinivas Ampati ◽  
Sarangapani Manda
Keyword(s):  
Spectral Analysis ◽  
Rat Model ◽  
Inflammatory Activity ◽  
Paw Edema ◽  
Mass Spectral Analysis ◽  
Thiourea Derivatives ◽  
Mass Spectral ◽  
H Nmr ◽  
Anti Inflammatory

In the present investigation we have synthesized a series of new 1-[3-(4-substitutedphenyl)-5-phenyl-4H-1,2,4-triazol-4-yl]urea and 1-[3-(4-substitutedphenyl)-5-phenyl-4H-1,2,4-triazol-4-yl]thiourea derivatives (4Ia - 4IId). The newly synthesised derivatives were characterized by using the data of IR,1H NMR and Mass Spectral analysis. Thus synthesised and characterized targetted compounds were further screened for their anti-inflammatory activity by using Carrageenan – induced paw edema rat model. Among all the newly synthesized derivatives, Compounds 4Ia-4Ic and Compounds 4IIa-4IId were reduced the inflammation very significantly (p<0.0001), thus these compounds showed promising anti-inflammatory activity and only one compound (4Id) showed moderate anti-inflammatory activity (p<0.05).

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 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.

scholarly journals Synthesis and Characterization of New Etodolac Derivatives with Possible Anti-Inflammatory Activity

2019 ◽  
Vol 28 (1) ◽  
pp. 107-113
Author(s):  
Omeed Muhsin Hassan ◽  
Susan Sarsam
Keyword(s):  
Ir Spectroscopy ◽  
Egg White ◽  
Inflammatory Activity ◽  
Synthesis And Characterization ◽  
Paw Edema ◽  
Ft Ir ◽  
Anti Inflammatory ◽  
Ft Ir Spectroscopy ◽  
Inflammatory Effect

A series of Etodolac hydrazone derivatives were synthesized and evaluated for their anti-inflammatory activity by using egg white induced paw edema method. All the synthesized target compounds were characterized by CHN- microanalysis, FT-IR spectroscopy and 1HNMR analysis. The synthesized target compounds (P1-P3) were found to be active in reducing paw edema thickness and their anti-inflammatory effect was comparable to that of the standard (Etodolac). Keywords: Etodolac hydrazone derivatives, anti-inflammatory, paw edemamethod.

scholarly journals TO SYNTHESIZE, CHARACTERIZATION AND PHARMACOLOGICAL EVALUATION OF NOVEL SUBSTITUTED ISATIN DERIVATIVES

2020 ◽  
Vol 9 (1) ◽  
Author(s):  
D B Joshi
Keyword(s):  
Schiff Bases ◽  
Picric Acid ◽  
Epileptic Seizures ◽  
Inflammatory Activity ◽  
Paw Edema ◽  
Standard Drug ◽  
Edema Volume ◽  
Rat Paw Edema ◽  
Anti Inflammatory ◽  
Rat Paw

Series of novel Schiff bases of Isatin the  equimolar amines and 5-Dicrboxymethyl (R=COO2Me) substituted isatins (1 mmol of each) were added to 96% w/w ethanol (20 mL) containing 8 drops of glacial acetic acid. The mixture was heated under reflux for 5 h and then cooled to room temperature. The resulting solid was collected by filtration, washed with cold ethanol and dried in open air. The derivatives thus prepared had sufficient analytical purity. anticonvulsant activity performed by method as Animals were weighed and numbered. Mice were divided into 7 groups of six animals each. Group 1 served as control which was treated with vehicle (2% v/v Tween 80), group 2 was treated with standard drug phenytoin (25 mg/kg, i.p.) and groups 3– 7 were treated with newly synthesized oxadiazole derivatives (25 mg/kg, i. p.). One hour after injection, the animals were subjected to electro shock through ear electrodes of 80 mA for 0.2 sec by electroconvulsiometer AND ANTI-inflammatory activity measured by Weigh the animals and number them. Mark the animals with picric acid for individual animal identification. Divide rats into 5 groups of 6 rats each. Note the initial paw volume of each rat by dipping just beyond tibio-tarsal junction by mercury displacement method. The pharmacological screening of the synthesized compounds showed anti convulsant activity ranging from 56.2 % to 76.3 % inhibition of epileptic seizures in mice, where as the standard drug Phenytoin showed 83.95 % inhibition of epileptic seizures in mice. The compound iiih4 from each group was found to be nearly potent to Phenytoin which is used as standard drug. Anti-inflammatory activity ranging from 31.09 to 63.11 % inhibition of rat paw edema volume after 3 hours, whereas the standard drug Indomethacin showed 62.06 % inhibition of rat paw edema volume after 4 hours.  The compound iiih3 was found to be nearly more potent then indomethacin which is used as standard drug Keywords: Isatin; Schiff bases; Anti convulsant activity; Anti-inflammatory activity; Isatin.

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, 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.

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