scholarly journals SYNTHESIS AND EVALUATION OF ANTI-INFLAMMATORY AND ANTIBACTERIAL ACTIVITIES OF SOME 1, 2-BENZISOXAZOLE DERIVATIVES

2016 ◽  
Vol 8 (4) ◽  
pp. 64 ◽  
Author(s):  
Sarath Sasikumar ◽  
Haripriya M. ◽  
Anjali T.
Keyword(s):  
Antibacterial Activity ◽  
Diclofenac Sodium ◽  
Analytical Techniques ◽  
Antibacterial Activities ◽  
Inflammatory Activity ◽  
Antibacterial Drug ◽  
Standard Drug ◽  
Good Antibacterial Activity ◽  
Anti Inflammatory ◽  
And Staphylococcus Aureus

Objective: A series of 1, 2-Benzisoxazole derivatives were synthesized and characterized by various analytical techniques like Melting point, Rf, FTIR, and NMR spectra.Methods: Structures of the compounds were elucidated and evaluated for anti-inflammatory activity by HRBC membrane stabilization method, antibacterial activity against Escherichia coli and Staphylococcus aureus by cup plate method.Results: The compounds 4a and 4e showed good anti-inflammatory activity compared with standard drug Diclofenac sodium and compounds 4b and 4d showed good antibacterial activity on compared with standard drug Gentamycin.Conclusion: These compounds may serve as future leads for anti-inflammatory and antibacterial drug discovery.

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 Comperative phyto toxicological and anti inflammatory effects of leaves extracts of holoptelea integrifolia

2018 ◽  
Vol 17 (2) ◽  
pp. 212-217
Author(s):  
Hina Yasin ◽  
Shaukat Khalid ◽  
Hina Abrar ◽  
Ghazala H Rizwani ◽  
Rehana Perveen ◽  
...  
Keyword(s):  
Aqueous Extract ◽  
Diclofenac Sodium ◽  
Medical Science ◽  
Inflammatory Activity ◽  
Albino Rats ◽  
High Dose ◽  
Inhibition Activity ◽  
Standard Drug ◽  
Etoac Extract ◽  
Anti Inflammatory

Objective: Plants play valuable role in the new drug discovery and significantly used to treat different diseases. Nowadays scientists are investigating the therapeutically active phytochemical constituents that are safe and producing lesser side effect in comparative to other standard drugs.Methods: The plant Holoptelea integrifolia is medicinally important and this study was carried out to evaluate the anti inflammatory activity of aqueous extract of the leaves of Holoptelea integrifolia in male albino rats wistar stain treated with acetic acid to induced paw edema.Results: Result indicated the significant anti-inflammatory activity while compared with standard drug (diclofenac sodium).Brine shrimp bioassay (cytotoxicity), phytotoxicity, insecticidal and enzyme inhibition activity was performed in different extracts of the leaves of H. integrifolia. Results of brime shrimp bioassay indicating positive lethality at high dose in BuOH and H2O only. While the results of phytotoxicity in all crude extracts displayed mild phytotoxicity(46.3 µg/ml) in high concentrations (1000 µg/ml) except H2O extract showed no phytotoxicity. Result of insecticidal activity revealed that BuOH extract were found more effective against Rhyzoperthadominica, the EtOH extract expressed major while EtOAC extract showed mild activity against Callosobruchusanalis. Aqueous extract possessed no insecticidal activity.Conclusion: Results of Urease inhibition activity suggested that EtOAC and BuOH extracts of this plant expressed no activity while EtOH and H2O possessed mild inhibiting activity.Bangladesh Journal of Medical Science Vol.17(2) 2018 p.212-217

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.

IN VITRO ANTI-INFLAMMATORY ACTIVITY OF METHANOLIC EXTRACT AND DIFFERENT FRACTIONS OF CENTELLA ASIATICA LEAVES BY PROTEIN DENATURATION

INDIAN DRUGS ◽  
2019 ◽  
Vol 56 (06) ◽  
pp. 86-89
Author(s):  
S Sharma ◽  
◽  
R. Trivedi ◽  
N. K. Choudhary
Keyword(s):  
Petroleum Ether ◽  
Skin Diseases ◽  
Methanolic Extract ◽  
Protein Denaturation ◽  
Diclofenac Sodium ◽  
Centella Asiatica ◽  
Inflammatory Activity ◽  
Standard Drug ◽  
Anti Inflammatory

Inflammation might be a complex organic reaction to a hazardous stimulant such as pathogens, or injured tissues and mainly causes itching, swelling, skin redness, warm and slight pain. Herbal drugs are widespread in India for their effectiveness, easy availability at low cost and provide low toxicity as compared to modern drugs. Centella asiatica is one of the oldest Ayurvedic medicinal plants, used in treatment of various skin diseases. The aim of our present research was to evaluate the in vitro anti-inflammatory activity of methanolic extract and different fractions of C. asiatica leaves. In protein denaturation method, the percentage inhibition for methanolic extract was observed to be 40.22%. The petroleum ether and n-butanol fraction of methanolic extract of C. asiatica were observed to exhibits 54.12 and 44.42% inhibition, respectively. Diclofenac sodium was used as a standard drug. In comparison with other fractions petroleum ether and n-butanol fractions showed best activity. The preliminary phytochemical studies of n-butanol fractions and n-butanol fractions showed the presence of terpenoids, flavonoids etc., which are used in the treatment of inflammation. Thus, we can call the latter as intense anti-inflammatory agent.

scholarly journals EVALUATION OF IN VITRO ANTI-INFLAMMATORY ACTIVITY OF CITRUS MACROPTERA MONTR

2020 ◽  
pp. 101-103
Author(s):  
SONAM BHUTIA
Keyword(s):  
In Vitro Model ◽  
Diclofenac Sodium ◽  
Test Sample ◽  
Scientific Data ◽  
Inflammatory Activity ◽  
Standard Drug ◽  
Reference Drug ◽  
Anti Inflammatory ◽  
Vitro Model

Objective: The use of naturally occurring medicines dependent on essential oils (EOs) is nowadays of great interest. In addition, within the human body, EO shows high efficacy as antioxidants and anti-inflammatory drugs. The present experiment was conducted to access the anti-inflammatory activity of EO obtained from the fruit peels of Citrus macroptera Montr. (Rutaceae) against the denaturation of protein in vitro model. Methods: The test sample (EO) was incubated under controlled laboratory conditions at varying concentrations with egg albumin and was subjected to absorbance determination for the anti-inflammatory property analysis. Diclofenac sodium was used as the standard reference drug for the experiment. Results: The results show a concentration-dependent inhibition of protein (albumin) denaturation by the test oil. This was concluded by comparing their IC50 average values. Citrus macroptera Montr. EO possessed IC50 average value 54.6+0.07 μg/mL, whereas that of diclofenac sodium was found to be 52.89+0.06 μg/ml. The result shows that the test oil is more effective than the standard drug. Conclusion: From the above experimental finding, it can be concluded that Citrus macroptera Montr. EO has significance anti-inflammatory effect against the denaturation of the protein in vitro model. The activity may be due to the presence of terpene polyphenolic component or some other active compound present in the oil. The provided information was first of its kind of knowledge to keep the scientific data for future reference.

scholarly journals Evaluation of analgesic and anti-inflammatory activity of Levocetirizine in albino rats

2019 ◽  
Vol 8 (8) ◽  
pp. 1805
Author(s):  
Dipti R. Sonawane ◽  
Jugalkishor B. Jaju ◽  
Ganesh R. Pawar ◽  
Punam A. Gosavi
Keyword(s):  
Analgesic Activity ◽  
Diclofenac Sodium ◽  
Inflammatory Activity ◽  
Hot Plate ◽  
Plate Method ◽  
Standard Drug ◽  
Group I ◽  
Anti Inflammatory ◽  
Rat Paw ◽  
Tail Clip

Background: Levocetirizine, the R-enantiomer of Cetirizine has pharmacokinetically and pharmacodynamically favourable characteristics, with rapid onset of action, high bioavailability, high affinity for and occupancy of the H1-receptor, limited distribution, minimal hepatic metabolism together with minimal side effects. Non-steroidal anti-inflammatory drugs (NSAIDs) have been used for many years for analgesic, anti-inflammatory, and more recently in the case of aspirin, antithrombotic purposes. Because of the significant side effect profiles of steroidal and NSAID medications, there is a greater interest in newer compounds such as antihistaminic drugs. This article will consider the potential or otherwise of the reported analgesic and anti-inflammatory effects of levocetirizine to enhance its effectiveness in the treatment of allergic disease with pain.Methods: Albino Wistar rats of either sex weighing 150-250 grams were used. For both Analgesic activity and Anti-inflammatory activity, 4 groups consisting of 6 animals per group were used. Group I: Control: 1% Gum acacia. 2ml/kg, Group II: Standard drug: Diclofenac sodium 4.5mg/kg; Group III: Test Drug 1: Levocetirizine 1mg/kg; Group IV: Test Drugs 2: Levocetirizine 1mg/kg+Diclofenac sodium 4.5mg/kg. Drugs were administered orally. For analgesic activity, Tail clip method and Hot plate method was used. For acute anti-inflammatory activity Carrageenan induced rat paw oedema method was used.Results: Levocetirizine, is found to have significant analgesic activity in rats (1 mg/kg dose) alone and in combination with Diclofenac Sodium in Haffner’s Tail Clip method and Eddy’s Hot Plate Method. Levocetirizine also has got prominent anti-inflammatory activity in acute models evidenced by percentage inhibition of acute rat paw oedema.Conclusions: Levocetirizine possess analgesic and acute anti-inflammatory activity alone and in combination with Diclofenac sodium.

scholarly journals EVALUATION OF IN VITRO ANTIDIABETIC AND ANTI-INFLAMMATORY ACTIVITIES OF LEAVES EXTRACT OF BOEHMERIA RUGULOSA

2018 ◽  
Vol 11 (9) ◽  
pp. 200
Author(s):  
Abha Shukla ◽  
Anchal Choudhary
Keyword(s):  
Protein Denaturation ◽  
Diclofenac Sodium ◽  
Significant Inhibition ◽  
Inflammatory Activity ◽  
Antidiabetic Activity ◽  
Standard Drug ◽  
Successive Extraction ◽  
Ic50 Value ◽  
Anti Inflammatory

Objective: The objective of the study is to evaluate in vitro antidiabetic and anti-inflammatory activity of different extracts of leaves of Boehmeria rugulosa by different methods.Methods: In vitro α-glucose and α-amylase were used for antidiabetic activity and lipoxygenase, and protein denaturation method of inhibition assays was used to measure anti-inflammatory activity. Successive extraction of leaves petroleum ether (PE), chloroform (CH), ethyl acetate (EA), acetone (AC), and ethanol (ETH) was performed, and extracts obtained from the extraction were applicable to these activities.Results: The AC extract of leaves shows significantly in vitro antidiabetic activity, and AC has offered significant result 470.07±0.65 μg/mL in the inhibition of α-glucosidase and also for α-amylase assay 698.15±1.71 μg/mL. Acarbose was used as standard. In lipoxidase method, AC had shown better results and in protein denaturation method EA shown the higher inhibition (78.06±0.5 μg/ml) than the other extracts. The standard drug diclofenac sodium also offered significant inhibition against lipoxidase enzyme method with IC50 value 21.76±1.29 μg/mL.Conclusion: These findings suggest that the AC and EA possess potent antidiabetic and anti-inflammatory activities in vitro conditions.

Synthesis and SAR Evaluation of Mercapto Triazolobenzothiazole

2021 ◽  
Vol 18 (4) ◽  
pp. 362-374
Author(s):  
Mamatha S.V ◽  
S.L. Belagali ◽  
Mahesh Bhat
Keyword(s):  
Antibacterial Activity ◽  
Biological Activities ◽  
Antibacterial Activities ◽  
Biological Properties ◽  
Biological Evaluation ◽  
Step Method ◽  
Good Antibacterial Activity ◽  
Anti Inflammatory ◽  
Mic Value

Background: Benzothiazoles possess a vast sphere of biological activities including anti- inflammatory, antibacterial activities whereas triazoles display various pharmacological properties including antimicrobial and antitubercular activities. Hence, triazole conjugated benzothiazole side-chain anticipating their interesting biological properties has been focused upon. Objective: The objective of the current work is synthesis and biological evaluation of a new series of benzothiazole appended triazole derivatives. Methods: The target compounds were prepared via a multi-step method involving the treatment of 2-amino benzothiazole with hydrazine followed by cyclization with carbon disulfide to give the corresponding triazol-2-thiol derivatives and then alkylation of these derivatives. All the synthesized compounds were characterized by FT-IR, Mass, 1H and 13C NMR spectra and were screened for their antibacterial, antioxidant, anti-inflammatory and anti-tubercular (anti-TB) activities in vitro. These molecules were also docked into the enoyl acyl carrier reductase (Inha, PDB ID-1ZID) in silico. Results: While all the synthesized compounds were active against M. tuberculosis at 50 μg/ml, the pyrrolidine and piperidine appended benzothiazolyltriazoles showed the superior activity (MIC values 12.5 to 1.6 μg/ml). Compound 5a (5-CH3 with piperidine), 5b (7-CH3 with piperidine) and 7b (7-CH3 with pyrrolidine) showed good antibacterial activity against Staphylococcus aureus with MIC value 31.25μg/ml, while compounds 7a (5-CH3 with pyrrolidine), 6b (7-CH3 with morpholine) and 8c (7-Br with pyridine) exhibited good antibacterial activity against E-coli with MIC value 62.5μg/ml. Compounds 7b (7-CH3 with pyrrolidine) and 5c (7-Br with piperidine) showed good anti-oxidant activities with IC50 values 93.25 and 82.25, respectively. Notably, these compounds were non-toxic to the normal cells even at high concentrations with IC50 value 238μg/ml. Conclusion: The compound 7b, a benzothiazolyltriazole having a pyrrolidine group (five membered ring) attached to two CH2 groups and methyl substituent at 7th position of the benzothiazole ring emerged as a novel and promising hit molecule that showed anti-TB, antimicrobial and antiinflammatory activities in vitro.

scholarly journals Synthesis, characterization and pharmacological evaluation of substituted phenoxy acetamide derivatives

2015 ◽  
Vol 69 (4) ◽  
pp. 405-415 ◽  
Author(s):  
Priyanka Rani ◽  
Dilip Pal ◽  
Rahul Hegde ◽  
Syed Hashim
Keyword(s):  
Analgesic Activity ◽  
Diclofenac Sodium ◽  
Inflammatory Activity ◽  
The Novel ◽  
Standard Drug ◽  
Antipyretic Activity ◽  
Paw Oedema ◽  
Anti Inflammatory ◽  
Rat Paw ◽  
Rat Paw Oedema

A novel series of 2-(substituted phenoxy)-N-(1,7,7-trimethylbicyclo[2.2.1]heptan-2-yl)acetamide and N-(2-bromocyclohexyl)-2-(substituted phenoxy)acetamide derivatives having cyclohexyl nucleus as common in both types were synthesized and assessed for their anti-inflammatory activity by a carrageenan induced rat paw oedema method, analgesic activity by Eddy?s hot plate method and antipyretic activity by brewer?s yeast induced pyrexia method. All the novel derivatives have been synthesized by the reaction of camphor and similar ketone having cyclohexane nucleus (e.g. 2-bromocyclohexanone) with ammonium carbonate and formic acid resulting in the formation of aromatic amines (1a-b). These amines on further chloroacetylation with chloroacetylchloride give compounds (2a-b). Compounds (2a-b) are converted to 2-(substituted phenoxy)-N-(1,7,7-trimethylbicyclo[2.2.1]heptan-2-yl) acetamide and N-(2-bromocyclohexyl)-2-(substituted phenoxy)acetamide derivatives on treatment with substituted phenol. Among the series 3a-f, 3i, 3k, 3l compounds showed significant anti-inflammatory activity as compared to the standard drug diclofenac sodium and also compound 3a-f, 3h, 3j, 3k exhibit significant analgesic activity as compared to the standard drug. Compounds 3a-f and 3k showed antipyretic activity nearly to the standard drug indomethacin. Compounds 3a-f and 3k possess anti-inflammatory, analgesic and antipyretic activities near to the standard.

scholarly journals SYNTHESIS OF 1-BENZOYL-3-PHENYL-1H-PYRAZOLE-4-CARBALDEHYDE AND EVALUATION OF THEIR ANTIOXIDANT AND ANTI-INFLAMMATORY ACTIVITY

2021 ◽  
pp. 48-52
Author(s):  
BONO NAGA SUDHA ◽  
N YELLA SUBBAIAH ◽  
MANCHALA MAHALAKSHMI
Keyword(s):  
Diclofenac Sodium ◽  
Radical Scavenging ◽  
Inflammatory Activity ◽  
Proton Nuclear Magnetic Resonance ◽  
Significant Activity ◽  
Mass Spectral Data ◽  
Standard Drug ◽  
Mass Spectral ◽  
Antioxidant Potency ◽  
Anti Inflammatory

Objective: The main objective of this study is to synthesize a series of 1-Benzoyl-3-phenyl-1H-pyrazole-4-carbaldehyde (4a-e) derivatives and evaluation of the synthesized compounds for their antioxidant and anti-inflammatory activity. Methods: A series of substituted acetophenones are condensed with hydrazides to the corresponding hydrazones which are subsequently cyclized by using vilsmier-Haack reaction to give final series of 1-Benzoyl-3-phenyl-1H-pyrazole-4-carbaldehyde (4a-e) derivatives respectively. All newly synthesized compounds were characterized on the basis of infrared, proton nuclear magnetic resonance and mass spectral data and screened for their antioxidant and anti-inflammatory activities. Results: In view of the significant biological activity profile of Pyrazole, the synthesized compounds (4a-e) were evaluated for their antioxidant potency by DPPH, Nitric oxide, Hydroxyl radical scavenging, and Hydrogen Peroxide method. Compounds 4c and 4e showed potent antioxidant activity then standard. Synthesized compounds were also screened for anti-inflammatory activity. Among all the molecules 4c, 4e, and 4d showed significant activity as compared to standard drug diclofenac sodium. Conclusion: in this study, we synthesized 1-Benzoyl-3-phenyl-1H-pyrazole-4-carbaldehyde (4a-e) derivatives. Further, these derivatives showed significant antioxidant and anti-inflammatory activity. Among them, two molecules 4c and 4e have shown near action to the standard.

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