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.

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 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.

Synthesis of Asymmetric 1-Thiocarbamoyl Pyrazoles as Potent Anti- Colon Cancer, Antioxidant and Anti-Inflammatory Agent

2019 ◽  
Vol 18 (15) ◽  
pp. 2117-2123 ◽  
Author(s):  
Dattatraya G. Raut ◽  
Sandeep B. Patil ◽  
Vikas D. Kadu ◽  
Mahesh G. Hublikar ◽  
Raghunath B. Bhosale
Keyword(s):  
Colon Cancer ◽  
Diclofenac Sodium ◽  
Radical Scavenging ◽  
Inflammatory Activity ◽  
Assay Method ◽  
Anticancer Activities ◽  
Cancer Society ◽  
Standard Drug ◽  
Anti Inflammatory

Background: Cancer is one of the leading diseases responsible for deaths in the society. According to the American cancer society, there will be 95,270 new cases of colon cancer in the U.S. in 2016. When a normal cell turns cancerous they develop into tumours, which produce various pro-inflammatory and inflammatory cytokines and chemokines that attract leukocytes to the site of growth. The main aim of this paper is to introduce readers about the increased number of cancer patient, effects of cancer and need of research on same. Methods: The target molecules were prepared by reacting pyrazolealdehyde with appropriate aromatic ketone by using polyethylene glycol (PEG-300) as green solvent and catalyst to yield chalcone. Furthermore, the reaction of chalcones with thiosemicabazide yields asymmetric 1-thiocarbamoyl pyrazoles. All the newly synthesized compounds were in vitro screened for their anticancer activities against Colon SW-620 by employing the sulforhodamine B (SRB) assay method. Also all the synthesized compounds tested for in vitro antioxidant and anti-inflammatory activity by using known literature methods. Results: Preliminary in vitro evaluation indicated that most of the compounds 4c, 4d and 4e possess distinct cytotoxicity profile against Colon SW-620 cell line compared to standard drug adriamycin. All the tested compounds showed good to excellent antioxidant activity against one or more reactive (H2O2, DPPH, SOR and NO) radical scavenging species. Additionally, all the synthesized compounds were screened for their in vitro antiinflammatory activity. Compounds 4a, 4b and 4e shows potent anti-inflammatory activity as compared to diclofenac sodium as a standard reference. Conclusion: New anti- Colon SW-620 cancer agents are the need of time, we trust that 1-thiocarbamoyl pyrazole derivatives 4c, 4d and 4e constitute an interesting template for the evaluation of new anticancer agent also antioxidant and anti-inflammatory work may provide an interesting insight for further development.

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 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.

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