Thiazole-Based Chalcone Derivatives as Potential Anti-inflammatory Agents: Biological Evaluation and Molecular Modelling

Background.: Inflammation is a multifactorial process reflecting response of the organismto various stimuli and is associated to a number of disorders such as arthritis, asthma and psoriasis, which require long-lasting or repeated treat-ment. Objective.: The aim of this paper is to evaluate the anti-inflammatory activity of previous synthesized thiazole-based chal-cone derivatives. Method.: Chalcones were synthesized via Cliazen-Schmidt condensation1-(4-methyl-2-alkylamino)thiazol-5-yl) ethanone with corresponding aromatic aldehyde. For the evaluation of possible anti-inflammatory activity carrageneen mouse paw edema was used. Results.: Eight out of thirteen tested chalcones showed anti-inflammatory activity in range of 51-55%. Prediction of toxicity revealed that these compounds are not toxic. Conclusion.: In general, it can be concluded that these compounds can be used for further modifications in order to develop more active and safe agents.

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

International Journal of Current Pharmaceutical Research ◽

10.22159/ijcpr.2018v10i4.28455 ◽

2018 ◽

Vol 10 (4) ◽

pp. 29 ◽

Cited By ~ 2

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.

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Synthesis and Biological Evaluation of Nonaprenylsulfates

Natural Product Communications ◽

10.1177/1934578x1300801124 ◽

2013 ◽

Vol 8 (11) ◽

pp. 1934578X1300801

Author(s):

Suryachandra R. Ravada ◽

Lakshmareddy Emani ◽

Ganeswara R. Mallula ◽

Trimurtulu Golakoti

Keyword(s):

Brine Shrimp ◽

Radical Scavenging ◽

Biological Evaluation ◽

Inflammatory Activity ◽

Synthetic Analogue ◽

Paw Edema ◽

Naturally Occurring ◽

Anti Oxidant ◽

Anti Inflammatory ◽

Synthesis And Biological Evaluation

A naturally occurring nonaprenylsulfate (1) and its synthetic analogue (2) were synthesized from substituted phenolic precursors in three steps with an overall yield of 40–45%. Both compounds exhibited potent anti-inflammatory activity against 5-lipoxygenase, and potent brine shrimp lethality. They also showed moderate anti-oxidant activity in the super oxide radical scavenging model. Nonaprenylsulfate (1) showed moderate inhibition of paw edema in Freund's Complete Adjuvant (FCA) induced model of arthritis, thus confirming its anti-inflammatory activity.

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Docking Studies, Synthesis and Biological Evaluation of β-aryl-β-hydroxy Propanoic Acids for Anti-inflammatory Activity

Medicinal Chemistry ◽

10.2174/1573406412666160907150247 ◽

2017 ◽

Vol 13 (2) ◽

pp. 186-195 ◽

Cited By ~ 3

Author(s):

Jelena Savic ◽

Sanda Dilber ◽

Marina Milenkovic ◽

Jelena Kotur-Stevuljevic ◽

Bojan Markovic ◽

...

Keyword(s):

Docking Studies ◽

Biological Evaluation ◽

Inflammatory Activity ◽

Anti Inflammatory ◽

Synthesis And Biological Evaluation

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ANTIULCER AND ANTI-INFLAMMATORY ACTIVITIES OF HYDROALCOHOLIC EXTRACTS OF STEM BARK AND LEAF OF ANOGEISSUS PENDULA EDGEW

INDIAN DRUGS ◽

10.53879/id.58.01.11950 ◽

2021 ◽

Vol 58 (01) ◽

pp. 41-46

Author(s):

Deeksha Singh ◽

◽

Amit Nayak ◽

Rakesh Yadav ◽

Uttam Singh Baghel ◽

...

Keyword(s):

Phenolic Compounds ◽

Stem Bark ◽

Inflammatory Activity ◽

Antiulcer Activity ◽

Paw Edema ◽

Ulcer Index ◽

Pylorus Ligation ◽

Anti Inflammatory ◽

Anogeissus Pendula

Anogeissus pendula Edgew has been reported to be used in gastric disorder even though no attempt has been made to evaluate the same. The present study was designed to evaluate the hydroalcoholic extracts of stem bark and leaves for in vivo acute antiulcer and anti-inflammatory activities. Antiulcer activity was studied by pylorus ligation induced ulcers while anti-inflammatory activities was studied by carrageenan induced paw edema. The extract of stem bark at 200 and 400 mg/kg b. w., significantly (P<0.05) reduced ulcer index whereas extracts of both stem bark and leaves significantly (P<0.001) reduced paw diameter at the fifth hour. The hydroalcholic extract of stem bark of A. pendula possesses more significant antiulcer and anti-inflammatory activity than the hydroalcholic extract of leaves may be due to the presence of higher amount of phenolic compounds.

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Anti-inflammatory activity and modulate oxidative stress of Bucida buceras in lipopolysaccharide-stimulated RAW 264.7 macrophages and Carrageenan-induced acute paw edema in rats

Journal of Medicinal Plants Research ◽

10.5897/jmpr2017.6334 ◽

2017 ◽

Vol 11 (12) ◽

pp. 239-252 ◽

Cited By ~ 3

Author(s):

B. Iloki Assanga Simon ◽

M. Lewis Luján Lidianys ◽

A. Gil-Salido Armida ◽

L. Lara Espinoza Claudia ◽

Fernandez Angulo Daniela ◽

...

Keyword(s):

Oxidative Stress ◽

Inflammatory Activity ◽

Raw 264.7 ◽

Paw Edema ◽

Raw 264.7 Macrophages ◽

Anti Inflammatory

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SYNTHESIS AND PRELIMINARY PHARMACOLOGICAL EVALUATION OF NEW NAPROXEN ANALOGUES HAVING 1, 2, 4-TRIAZOLE-3-THIOL

International Journal of Pharmacy and Pharmaceutical Sciences ◽

10.22159/ijpps.2017v9i7.18273 ◽

2017 ◽

Vol 9 (7) ◽

pp. 66

Author(s):

Monther F. Mahdi ◽

Noor H. Naser ◽

Nethal H. Hammud

Keyword(s):

Aromatic Aldehydes ◽

Heterocyclic Ring ◽

Inflammatory Activity ◽

Control Group ◽

Paw Edema ◽

Dose Equivalent ◽

Edema Model ◽

Anti Inflammatory ◽

Derivatives Of

Objective: The objective of this search was to synthesize a new naproxen analogues having a 1,2,4-triazole-3-thiol heterocyclic ring, and preliminary pharmacological assessment of the anti-inflammatory activity of the synthesized compounds. Methods: The synthesis of naproxen analogues that having 1,2,4-triazole-3-thiol heterocyclic ring occur through esterification of naproxen, and then its reaction with hydrazine hydrate, and carbon disulfide, finally different aromatic aldehydes reacted with triazole derivatives of naproxen containing amino group to produce schiff bases.Results: In vivo acute anti-inflammatory activity of the synthesize compounds (Va-Vd) was evaluated in rats using egg-white induced edema model of inflammation in a dose equivalent to (50 mg/kg) of naproxen. All tested compounds were produced a significant reduction in paw edema with respect to the effect of propylene glycol 50% v/v (control group). Compound Vd produced superior anti-inflammatory activity compared to naproxen.Conclusion: The results obtained in this work give evidence about the valid synthesis of 1,2,4 triazole-3-thiol derivatives of naproxen, which reacted with different aldehydes to yield several schiff bases. The incorporation of benzaldehyde possess para-electron donating group (para-hydroxyl benzaldehyde) will increase the anti-inflammatory activity of naproxen.

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Evaluation of analgesic and anti-inflammatory activity of ethanolic extract of Enhydra fluctuans on male wistar rats

Journal of Applied Pharmaceutical Research ◽

10.18231/joapr.2021.9.1.37.42 ◽

2021 ◽

Vol 9 (1) ◽

pp. 1-7

Author(s):

Kishor Kumar Roy ◽

Md. Kabirul Islam Mollah ◽

Md. Masud Reja ◽

Dibyendu Shil ◽

Ranjan Kumar Maji

Keyword(s):

Wistar Rats ◽

Pain Threshold ◽

Ethanolic Extract ◽

Inflammatory Activity ◽

Paw Edema ◽

Hot Plate ◽

Plate Method ◽

Traditional System ◽

Male Wistar Rats ◽

Anti Inflammatory

Enhydra fluctuations an edible semi-aquatic vegetable plant are widely used in the traditional system of medicine. Ethanolic extract of Enhydra fluctuans was screened for analgesic & anti-inflammatory activity. Analgesic activity was evaluated by the hot plate method and anti-inflammatory activity was evaluated by formalin induce paw edema in Wistar rats (male). Ethanolic extract dose of 300 mg/kg reduce formalin induce paw inflammation and also increased the pain threshold in rats evidenced by hot plate method. The experimental results concluded that Enhydra fluctuans have significant analgesic and anti-inflammatory activity may due to flavonoid and phenolic compound content.

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Anti-inflammatory activity of theophylline on carrageenan-induced paw edema in male wistar rats

International Journal of Basic & Clinical Pharmacology ◽

10.5455/2319-2003.ijbcp20130612 ◽

2013 ◽

Vol 2 (3) ◽

pp. 298 ◽

Cited By ~ 2

Author(s):

K Srinivasa ◽

BVS Chandrasekhar ◽

J Srinivasa

Keyword(s):

Wistar Rats ◽

Inflammatory Activity ◽

Paw Edema ◽

Male Wistar Rats ◽

Anti Inflammatory

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Scientific Evaluation of anti-inflammatory potential of Macrotyloma uniflorum seeds extracts

International Journal of Research in Pharmaceutical Sciences ◽

10.26452/ijrps.v11ispl4.4393 ◽

2020 ◽

Vol 11 (SPL4) ◽

pp. 1883-1888

Author(s):

Anandarajagopal K ◽

Abdullah Khan ◽

Sugalia S ◽

Bama Menon ◽

Tan Ching Siang ◽

...

Keyword(s):

Antioxidant Properties ◽

Water Extract ◽

Ethanol Extract ◽

Inflammatory Activity ◽

Leguminous Plant ◽

Paw Edema ◽

Reference Drug ◽

Macrotyloma Uniflorum ◽

Phenolic Constituents ◽

Anti Inflammatory

Phytochemicals possessing the antioxidant properties naturally present in food attract a greater interest to healthcare researchers due to their desirable health effects on human health as they can be explored for protection against oxidative deterioration. Macrtotyloma uniflorum is a leguminous plant belonging to the family Fabaceae and commonly known as Horse gram. Aqueous and ethanol extracts of seeds of Macrotyloma uniflorum were evaluated for their anti-inflammatory effects using the scientific protocol on experimental rats. Extraction was carried out using the cold maceration method, and the anti-inflammatory activity was evaluated using a digital plethysmometer in the experimental rats injected with carrageenan to produce paw edema. Preliminary phytochemical studies confirmed the presence of various bioactive compounds such as alkaloids, glycosides, carbohydrates, proteins and amino acids, terpenoids, tannins, and phenolic compounds in both extracts while flavonoids were found only in ethanol extract. Both extracts of M. uniflorum seeds (200 mg/ml) significantly (p<0.01) reduced the paw edema volume induced by carrageenan. The ethanol extract of M. uniflorum seeds exhibited more potent anti-inflammatory activity than water extract, that might be due to the presence of flavonoids in ethanol extract. The activity of the extracts was compared with diclofenac sodium (10mg/kg b.wt.) as a reference drug. From the results, it may be suggested that the antioxidative potential of phenolic constituents and flavonoids is the primary factors for the anti-inflammatory activity of M. uniflorum seeds extracts.

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