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 and biological evaluation of some 4-(1H-indol-3-yl)-6-phenyl-1,2,3,4-tetrahydropyrimidin-2-ones/thiones as potent anti-inflammatory agents

2008 ◽  
Vol 58 (4) ◽  
pp. 467-477 ◽  
Author(s):  
Mohammad Amir ◽  
Sadique Javed ◽  
Harish Kumar
Keyword(s):  
Lipid Peroxidation ◽  
Biological Evaluation ◽  
Inflammatory Activity ◽  
Test Results ◽  
Mass Spectral Data ◽  
Standard Drug ◽  
Mass Spectral ◽  
H Nmr ◽  
Anti Inflammatory ◽  
Synthesis And Biological Evaluation

Synthesis and biological evaluation of some 4-(1H-indol-3-yl)-6-phenyl-1,2,3,4-tetrahydropyrimidin-2-ones/thiones as potent anti-inflammatory agents Twelve new 4-(1H-indol-3-yl)-6-phenyl-1,2,3,4-tetrahydropyrimidin-2-ones/thiones (7-18) have been synthesized by reacting 1-aryl-3-(1H-indol-3-yl)-2-propen-1-one with urea and thiourea in ethanolic potassium hydroxide. Their structures have been confirmed by IR, 1H NMR and mass spectral data. The compounds were tested for their anti-inflammatory activity. Test results revealed that compounds showed 49.5 to 70.7% anti-inflammatory activity where-as the standard drug ibuprofen showed 86.4% activity at the same oral dose. Four compounds, 4-(1H-indol-3-yl)-6-(4-chlorophenyl)-1,2,3,4-tetrahydropyrimidin-2-one (8), 4-(1H-indol-3-yl)-6-(4-methylphenyl)-1,2,3,4-tetrahydropyrimidin-2-one (10), 4-(1H-indol-3-yl)-6-(4-chlorophenyl)-1,2,3,4-tetrahydropyrimidin-2-thione (14), 4-(1H-indol-3-yl)-6-(4-methylphenyl)-1,2,3,4-tetrahydropyrimidin-2-thione (16), that showed significant anti-inflammatory activity were selected to study their ulcerogenic and lipid peroxidation activities. All tested compounds showed significant reduction in the ulcerogenic potential and lipid peroxidation compared to the standard drug ibuprofen.

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.

scholarly journals Synthesis and Anti-inflammatory Activity of Some Novel 2,4-Diaryl-3,5-bis(arylimino)-1,2,4-thiadiazolidine Derivatives

2009 ◽  
Vol 6 (2) ◽  
pp. 495-503 ◽  
Author(s):  
P. Venkatesh ◽  
S. N. Pandeya
Keyword(s):  
Diclofenac Sodium ◽  
Inflammatory Activity ◽  
Second Step ◽  
Paw Edema ◽  
Mass Spectral Data ◽  
Mass Spectral ◽  
Methoxy Groups ◽  
Anti Inflammatory ◽  
Sar Study ◽  
New Compounds

A series of some novel 2,4-diaryl-3,5-bis(arylimino)-1,2,4-thiadiazolidine derivatives were synthesized and evaluated for anti-inflammatory activity. In the SAR study, the phenyl ring on 3 and 4 position of 1,2,4-thiadiazolidine ring substituted with chloro, nitro and methoxy groups showed better activity. The title compounds were synthesized from two steps; the first step involved the synthesis of diaryl substituted thioureas then, it was cyclised to give the 1,2,4-thiadiazole system in the presence of oxidizing agent (hydrogen peroxide and concentrated hydrochloric acid) in the second step. The purity of the synthesized compounds were judged by their C, H and N analysis and the structure was analyzed on the basis of IR, H1NMR, C13NMR and Mass spectral data. The anti-inflammatory activity of new compounds was determined by λ-Carrageenan induced mice paw edema method using diclofenac sodium as a standard. Among the compounds tested four compounds, B2 (2,4-diphenyl-3,5-bis(3-nitrophenylimino)-1,2,4-thiadiazolidine), B4 (2,4-diphenyl-3,5-bis(3-chlorophenylimino)-1,2,4-thiadiazolidine), B6 (2,4-diphenyl-3,5-bis(4-methoxyphenylimino)-1,2,4-thiadiazolidine) and B7 (2,4-diphenyl-3,5-bis (2-methoxyphenylimino)-1,2,4-thiadiazolidine) were the most active compounds in these series.

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

scholarly journals Quinazoline-containing Hydrazydes of Dicarboxylic Acids and Products of Their Structural Modification: A Novel Class of Anti-inflammatory Agents

2021 ◽  
Vol 68 (2) ◽  
pp. 395-403
Author(s):  
Nataliia Krasovska ◽  
Viktor Stavytskyi ◽  
Inna Nosulenko ◽  
Oleksandr Karpenko ◽  
Oleksii Voskoboinik ◽  
...  
Keyword(s):  
Chemical Modification ◽  
Spectral Data ◽  
1H Nmr ◽  
Structural Modification ◽  
Dicarboxylic Acids ◽  
Inflammatory Activity ◽  
Mass Spectral Data ◽  
Mass Spectral ◽  
Anti Inflammatory ◽  
Amide Fragment

The synthesis of hydrazides formed by quinazolin-4(3H)-ylidenehydrazine and dicarboxylic acids, as well as their further modification are described in the present manuscript. It was shown that above-mentioned hydrazides may be obtained via acylation of initial quinazolin-4(3H)-ylidenehydrazine by corresponding acylhalides, cyclic anhydrides and imidazolides of dicarboxylic acids monoesters. Obtained hydrazides were converted into [1,2,4]triazolo[1,5-с]quinazolines that were used as initial compounds for chemical modification aimed to the introduction of amide fragment to the molecule. The IR, 1H NMR and chromato-mass spectral data of obtained compounds were studied and discussed. Obtained substances were studied for anti-inflammatory activity using carrageenan-induced paw inflammation model. Amides of ([1,2,4]triazolo[1,5-с]quinazoline-2-yl)alkyl carboxylic acids were detected as promising class of anti-inflammatory agents for further purposeful synthesis and profound study of anti-inflammatory activity.

scholarly journals Synthesis, Anti-inflammatory Activity and in silico Studies of Some Novel Morpholine Based Carboxamides

2020 ◽  
Vol 32 (4) ◽  
pp. 901-906
Author(s):  
Premanand M. Honavar ◽  
Vasantha Kumar ◽  
P. Nikhil ◽  
Naveen Kumar ◽  
S. Sreenivasa ◽  
...  
Keyword(s):  
Inflammatory Activity ◽  
Mass Spectral Data ◽  
Mass Spectral ◽  
Rat Paw Edema ◽  
Amide Derivatives ◽  
In Silico Studies ◽  
Anti Inflammatory ◽  
Docking Interaction ◽  
Rat Paw ◽  
Aromatic Heterocyclic

Two series of carboxamides were synthesized from 3-fluoro-4-morpholinoaniline and different substituted aromatic/heterocyclic carboxylic acids. All the compounds were characterized by IR, 1H NMR, 13C NMR and mass spectral data. The newly synthesized amide derivatives were screened for anti-inflammatory activity by following carrageenan induced rat paw edema method. Among the compounds screened, compound 6e was found to be highly potent. Molecular docking interaction of active compounds revealed that effective binding was observed in the pocket of COX-I and COX-II proteins.

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.

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.

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