scholarly journals Synthesis and Anti-Inflammatory Activity of New Alkyl-Substituted Phthalimide 1H-1,2,3-Triazole Derivatives

2012 ◽  
Vol 2012 ◽  
pp. 1-7 ◽  
Author(s):  
Shalom Pôrto de Oliveira Assis ◽  
Moara Targino da Silva ◽  
Ronaldo Nascimento de Oliveira ◽  
Vera Lúcia de Menezes Lima
Keyword(s):  
Cycloaddition Reaction ◽  
Inflammatory Activity ◽  
Dipolar Cycloaddition ◽  
Terminal Alkynes ◽  
Triazole Derivatives ◽  
Inflammatory Agent ◽  
Anti Inflammatory ◽  
The Right

Four new 1,2,3-triazole phthalimide derivatives with a potent anti-inflammatory activity have been synthesized in the good yields by the 1,3-dipolar cycloaddition reaction fromN-(azido-alkyl)phthalimides and terminal alkynes. The anti-inflammatory activity was determined by injecting carrageenan through the plantar tissue of the right hind paw of Swiss white mice to produce inflammation. All the compounds3a–cand5a–cexhibited an important anti-inflammatory activity; the best activity was found for the compounds3band5c, which showed to be able to decrease by 69% and 56.2% carrageenan-induced edema in mice. These compounds may also offer a future promise as a new anti-inflammatory agent.

Synthesis of 1,4-Disubstituted 1H-1,2,3-Triazoles from 4-(1-Adamantyl)benzyl Azide through a 1,3-Dipolar Cycloaddition Reaction

Synlett ◽  
2018 ◽  
Vol 29 (20) ◽  
pp. 2685-2688
Author(s):  
Dahmane Tebbani ◽  
Artur Silva ◽  
Oussama Hocine
Keyword(s):  
Copper Catalyst ◽  
Cycloaddition Reaction ◽  
Dipolar Cycloaddition ◽  
Terminal Alkynes ◽  
Triazole Derivatives

A series of new 1,4-disubstituted 1H-1,2,3-triazole derivatives were synthesized by an efficient copper-catalyzed 1,3-dipolar cyclo­addition reaction of 4-(1-adamantyl)benzyl azide with several terminal alkynes. The copper catalyst was used to provide 1,4-disubstituted 1,2,3-triazoles regioselectively in good yields.

Copper-catalyzed Convenient Synthesis and SAR Studies of Substituted-1,2,3-triazole as Antimicrobial Agents

2018 ◽  
Vol 16 (1) ◽  
pp. 3-10
Author(s):  
Aniket P. Sarkate ◽  
Kshipra S. Karnik ◽  
Pravin S. Wakte ◽  
Ajinkya P. Sarkate ◽  
Ashwini V. Izankar ◽  
...  
Keyword(s):  
Antimicrobial Activity ◽  
Antifungal Activity ◽  
Antimicrobial Agents ◽  
Cycloaddition Reaction ◽  
Dipolar Cycloaddition ◽  
One Pot ◽  
Triazole Derivatives ◽  
Sar Studies ◽  
Convenient Synthesis ◽  
Antibacterial And Antifungal

Background:A novel copper-catalyzed synthesis of substituted-1,2,3-triazole derivatives has been developed and performed by Huisgen 1,3-dipolar cycloaddition reaction of azides with alkynes. The reaction is one-pot multicomponent.Objective:We state the advancement and execution of a methodology allowing for the synthesis of some new substituted 1,2,3-triazole analogues with antimicrobial activity.Methods:A series of triazole derivatives was synthesized by Huisgen 1,3-dipolar cycloaddition reaction of azides with alkynes. The structures of the synthesized compounds were elucidated and confirmed by 1H NMR, IR, MS and elemental analysis. All the synthesized compounds were tested for their antimicrobial activity against a series of strains of Bacillus subtilis, Staphylococcus aureus and Escherichia coli for antibacterial activity and against the strains of Candida albicans, Aspergillus flavus and Aspergillus nigar for antifungal activity, respectively.Results and Conclusion:From the antimicrobial data, it was observed that all the newly synthesized compounds showed good to moderate level of antibacterial and antifungal activity.

scholarly journals Green ultrasound-assisted three-component click synthesis of novel 1H-1,2,3-triazole carrying benzothiazoles and fluorinated-1,2,4-triazole conjugates and their antimicrobial evaluation

2017 ◽  
Vol 67 (3) ◽  
pp. 309-324 ◽  
Author(s):  
Nadjet Rezki ◽  
Mohamed Reda Aouad
Keyword(s):  
Antimicrobial Activity ◽  
Cycloaddition Reaction ◽  
Dipolar Cycloaddition ◽  
Terminal Alkynes ◽  
One Pot ◽  
Alkyl Aryl ◽  
Antimicrobial Evaluation ◽  
Ultrasound Assisted ◽  
Click Synthesis

AbstractThe present study describes an efficient and ecofriendly, ultrasound, one-pot click cycloaddition approach for the construction of a novel series of 1,4-disubstituted-1,2,3-triazoles tethered with fluorinated 1,2,4-triazole-benzothiazole molecular conjugates. It involved three-component condensation of the appropriate bromoacetamide benzothiazole, sodium azide and 4-alkyl/aryl-5-(2-fluorophenyl)-3-(prop-2-ynylthio)-1,2,4-triazoles4a-ethrough a Cu(I)-catalyzed 1,3-dipolar cycloaddition reaction. This approach involvesin situgeneration of azidoacetamide benzothiazole, followed by condensation with terminal alkynes in the presence of CuSO4/Na-ascorbate in aqueous DMSO under both conventional and ultrasound conditions. Some of the designed 1,2,3-triazole conjugates6a-owere recognized for their antimicrobial activity against some bacterial and fungal pathogenic strains.

scholarly journals SYNTHESIS NEW POTENTIAL ANTI-INFLAMMATORY AGENT SODIUM SALT OF PENTAGAMAVUNON-0

2010 ◽  
Vol 4 (3) ◽  
pp. 180-185
Author(s):  
Enade Perdana Istyastono ◽  
Rr. Sri Untari Siwi S.M.P ◽  
Andreas Asdi Utama ◽  
Supardjan A.M
Keyword(s):  
Inflammatory Activity ◽  
Physiological Changes ◽  
Solubility In Water ◽  
Curcumin Analogues ◽  
Inflammatory Agent ◽  
Curcumin Derivatives ◽  
Inflammatory Drugs ◽  
Anti Inflammatory ◽  
Living Tissues ◽  
Anti Inflammation

Inflammation is the response of living tissues to injury. The process affects physiological changes such as erythema, edema, asthma and fever. Non-steroid Anti-inflammatory Drugs (NSAIDs) have been developed since they could inhibit inflammation process because of its ability to inhibit biosynthesis of prostaglandin, one of inflammation mediators, through inhibition of cyclooxigenase (COX) enzymes. Molecules, which have been reported having anti-inflammatory activity, for example, are curcumin, some curcumin derivatives and curcumin analogues. One of curcumin analogues that has been  developed is pentagamavunon-0 (PGV-0) whose IUPAC name is 2,5-bis(4'-hidroxy-3'-methoxy-benzylidene)cyclo-pentanone. But PGV-0, which is like curcumin, practically insoluble in water, so it causes problems in the development. The aim of this research is to synthesize a derivative of PGV-0, a natrium salt of PGV-0 (natrium pentagamavunonate-0/Na-pentagamavunonate-0), which is hoped to have a better anti-inflammatory activity and solubility in water than PGV-0. PGV-0 was synthesized by reacting vanillin and cyclopentanone catalized by acid. Na-pentagamavunonate-0 was synthesized with PGV-0 as a starting material using an appropriate method. This research was able to synthesize new compound that was estimated as a natrium salt of PGV-0 (natrium pentagamavunonate-0/Na-pentagamavunonate-0).   Keywords: Curcumin, PGV-0, Na-pentagamavunonate-0, anti-inflammation

Anti-Inflammatory Activity of Ethanol Extract of Marine Sponge Petrosia Sp. by Supression the Level of Tumor Necrosis Factor-alpha

2021 ◽  
pp. 4435-4439
Author(s):  
Adryan Fristiohady ◽  
Muhammad Hajrul Malaka ◽  
Andi Rizqa Wahyuni Safitri ◽  
Dewo Diha ◽  
Saripuddin Saripuddin ◽  
...  
Keyword(s):  
Inflammatory Process ◽  
Oral Treatment ◽  
Ethanol Extract ◽  
The Body ◽  
Inflammatory Activity ◽  
Inflammatory Agent ◽  
Edema Volume ◽  
Group I ◽  
Tnf Α ◽  
Anti Inflammatory

Inflammation is the host's protective response to any stimulus that harms the body. Excessive inflammatory process causes tissue damage. Therefore, an anti-inflammatory agent is needed. The use of natural ingredients, especially sea sponges, is an option to reduce the side effects of anti-inflammatory agents. This utilization is related to the discovery of new agents. So, we tested the effect of the ethanol extract of Petrosia sp. as an anti-inflammatory agent. Animal induced with 1% carrageenan and left for 1 hour. After that the animals were divided into 6 groups (n = 4) and given oral treatment, namely: Group I (normal group); Group II (negative group); Group III (ethanol extract of Petrosia sp. Concentration of 0.05mg/ml); Group IV (ethanol extract of Petrosia sp. Concentration 0.1mg/ml); Group V (ethanol extract of Petrosia sp. Concentration 0.2mg/ml); and Group VI (positive group, Diclofenac Sodium). After 1 hour, the animals were measured for edema volume and plasma TNF-α levels. Based on the research conducted, the ethanol extract of Petrosia sp. decreased edema volume and plasma TNF-α levels in inflammatory mice. The concentration of 0.2mg/mL had a significant effect on the negative control used (p <0.05). On the other hand, Petrosia sp. indicates the presence of alkaloids, flavonoids, and steroids. They may play an important role in the anti-inflammatory process. Thus, it can be concluded that the ethanol extract of Petrosia sp. has anti-inflammatory activity.

scholarly journals EDEMA-REDUCING ACTIVITY OF SARGASSUM CRASSIFOLIUM Β-GLUCAN (LAMINARAN) ON EDEMA-INDUCED RATTUS NORVEGICUS

2017 ◽  
Vol 10 (7) ◽  
pp. 311 ◽  
Author(s):  
Anies Chamidah ◽  
Asep A Prihanto ◽  
Hardoko Hardoko
Keyword(s):  
Rattus Norvegicus ◽  
Brown Algae ◽  
Inflammatory Activity ◽  
Acid Extract ◽  
Inflammatory Agent ◽  
Reducing Activity ◽  
Anti Inflammatory ◽  
Leg Edema

Objectives: The aim of this study is to investigate anti-inflammatory activity of β-glucan (laminaran) of brown algae, Sargassum crassifolium which was extracted by using two different methods, β-glucan laminaran acid extract (LAE) and laminaran modified extract (LME).Methods: β-glucan (laminaran) of brown algae, S. crassifolium have been extracted using two different methods, namely, β-glucan LAE and LME. The edema reducing activity of the extracts was investigated with carrageenan- induced leg edema male of Rattus norvegicus as a model.Results: The swelling of edema was strongly inhibited by the treatment of LME with a percentage of 81.62% after 3rd hr. It also found that the size of edema were inhibited by all treatments with the value ranging from 25.49% to 81.68%. Smallest edema size was found on LME treatment, with a size of 0.68±0.09 mm where the control was about 0.92 mm. Furthermore, all β-glucan-treated mice showed lower edema size compared to control.Conclusion: It was obvious that all type of laminaran had anti-inflammatory activity. LME is the best method for production of β-glucan (laminaran) with high anti-inflammatory activity. Hence, in this study, we reported a new anti-inflammatory agent derived from S. crassifolium.

scholarly journals ANTI-INFLAMMATORY ACTIVITY OF METHANOL EXTRACT OF NIEBUHRIA APETALA (ROTH) DUNN – IN VITRO MODELS

2019 ◽  
pp. 278-281
Author(s):  
RAJESH A ◽  
DOSS A ◽  
TRESINA PS ◽  
MOHAN VR
Keyword(s):  
Methanol Extract ◽  
Protein Denaturation ◽  
In Vitro Models ◽  
Inflammatory Activity ◽  
Membrane Stabilization ◽  
Standard Drug ◽  
Inflammatory Agent ◽  
Potential Source ◽  
Anti Inflammatory

Objective: The objective of this study was to determine the anti-inflammatory activity of methanol extract of Niebuhria apetala and its possible mechanism of action. Methods: Methanol extract of Niebuhria apetala leaf (NAL) was assessed for its anti-inflammatory activity by in vitro methods. Using albumin denaturation assay, proteinase inhibitory activity, membrane stabilization, and antilipoxygenase activity at different concentrations, in vitro anti-inflammatory activity was estimated. The standard drug used for this purpose was aspirin. Results: Methanol extract NAL at a concentration range of 100–500 μg/ml significant (p<0.01) protects the heat-induced protein denaturation. At the concentration of 500 mg/ml, NAL showed significant (p<0.01) inhibition of protease inhibitory action. Heat-induced hemolysis of erythrocyte, hypotonicity-induced hemolysis, and lipooxygenase activity were significant (p<0.01) inhibited at the concentration of 500 μg/ml. Conclusion: Finally, the present study indicates that methanol extract of Niebuhria apetala can be a potential source of anti-inflammatory agent.

scholarly journals Piper cubebaL. Methanol Extract Has Anti-Inflammatory Activity Targeting Src/Syk via NF-κB Inhibition

2019 ◽  
Vol 2019 ◽  
pp. 1-8 ◽  
Author(s):  
Nurinanda Prisky Qomaladewi ◽  
Nur Aziz ◽  
Mi-Yeon Kim ◽  
Jae Youl Cho
Keyword(s):  
Inflammatory Activity ◽  
No Production ◽  
Immune Functions ◽  
Rt Pcr ◽  
Adaptive Immune ◽  
Inflammatory Agent ◽  
Inflammatory Mechanism ◽  
Gene Reporter Assay ◽  
Anti Inflammatory ◽  
Luciferase Gene Reporter Assay

Piper cubebaL. is a plant in the Piperaceae family that is generally found in tropical countries and acts as an antioxidant and anti-inflammatory agent. Unfortunately, the molecular mechanism of the anti-inflammatory activity has not been fully investigated. In this study, we elucidated the anti-inflammatory mechanism by focusing on NF-κB signaling, which is considered a prototypical inflammatory signaling pathway in both innate and adaptive immune functions. Cellular activity and the molecular target of Pc-ME were identified in macrophage RAW264.7 cells and HEK293T cells by assessing NO production, cytokine expression by RT-PCR, luciferase gene reporter assay, and protein regulation in cytoplasm by Western blot upon NF-κB activation. Pc-ME reduced NO production without any cell toxicity; inhibited expression of proinflammatory cytokines such as iNOS and IL-6; downregulated NF-κB activation mediated by both MyD88 and TRIF; and diminished the phosphorylation of IκBα, IKKα/β, Akt, p85, Src, and Syk. Pc-ME inhibited Syk and Src autophosphorylation during overexpression in HEK cells, which confirmed our hypothesis that Syk and Src were signaling targets of Pc-ME. These findings indicate thatPiper cubebaL. has anti-inflammatory activity by targeting Src/Syk in the NF-κB pathway.

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