Synthesis and Anti-Inflammatory Effect of Some More New Fluorinated 3-Substituted Amino/ 3,5-Diamino-1,2,4-Triazine Derivatives as Lamotrigine Analogs

2019 ◽  
Vol 16 (1) ◽  
pp. 165-172 ◽  
Author(s):  
Mohammed S.T. Makki ◽  
Reda M. Abdel-Rahman ◽  
Abdulrahman Salim Alharbi
Keyword(s):  
Spectral Data ◽  
Elemental Analysis ◽  
Biological Activities ◽  
Inflammatory Activity ◽  
The Novel ◽  
New Targets ◽  
Triazine Derivatives ◽  
Anti Inflammatory ◽  
Inflammatory Effect

Aim and Objective: It is known that the Lamotrigine drug has anti-inflammatory activity. So it was the goal to prepare similar compounds containing fluorine atoms (fluorine-substituted 3,5-diamino-6-aryl- 1,2,4-triazines) as Lamotrigine drug analogs to evaluate them as an anti-inflammatory. Materials and Methods: The novel fluorine substituted 3,5-diamino-6-aryl-1,2,4-triazines as new Lamotrigine analogs were prepared via aminolysis and/ or ammonolysis of the corresponding 3-thioxo-6-aryl-1,2,4-triazin- 5-ones in ethanolic media. </P><P> Results: All the new targets were deduced upon their elemental analysis and spectral data as well as screened as anti-inflammatory agents, where we found that the fluorinated systems 15 and 9-11 exhibited high and more activity. Conclusion: Simple routes to synthesize some more novel fluorinated Lamotrigine analogs have been reported. The new targets exhibited high and moderate anti-inflammatory probes. Presence of both amino and CF3 groups caused high biological activities of these compounds were studied.

scholarly journals A Review on the Anti-Inflammatory Activity of Pomegranate in the Gastrointestinal Tract

2013 ◽  
Vol 2013 ◽  
pp. 1-11 ◽  
Author(s):  
Elisa Colombo ◽  
Enrico Sangiovanni ◽  
Mario Dell'Agli
Keyword(s):  
Gastrointestinal Tract ◽  
Clinical Studies ◽  
Intestinal Tract ◽  
Biological Activities ◽  
Inflammatory Activity ◽  
Beneficial Effects ◽  
Anti Inflammatory ◽  
Gastro Intestinal Tract ◽  
Inflammatory Effect

Several biological activities of pomegranate have been widely described in the literature, but the anti-inflammatory effect in the gastrointestinal tract has not been reviewed till now. The aim of the present paper is to summarize the evidence for or against the efficacy of pomegranate for coping with inflammatory conditions of the gastro-intestinal tract. The paper has been organized in three parts: (1) the first one is devoted to the modifications of pomegranate active compounds in the gastro-intestinal tract; (2) the second one considering the literature regarding the anti-inflammatory effect of pomegranate at gastric level; (3) the third part considers the anti-inflammatory effect of pomegranate in the gut.In vivostudies performed on the whole fruit or juice, peel, and flowers demonstrate antiulcer effect in a variety of animal models. Ellagic acid was the main responsible for this effect, although other individual ellagitannins could contribute to the biological activity of the mixture. Different preparations of pomegranate, including extracts from peels, flowers, seeds, and juice, show a significant anti-inflammatory activity in the gut. No clinical studies have been found, thus suggesting that future clinical studies are necessary to clarify the beneficial effects of pomegranate in the gastrointestinal tract.

Synthesis and Biological Activities of 1,2,4-Triazine Derivatives

2014 ◽  
Vol 1033-1034 ◽  
pp. 283-286 ◽  
Author(s):  
Ri Hong Tan
Keyword(s):  
Elemental Analysis ◽  
Biological Activities ◽  
H Nmr ◽  
Triazine Derivatives ◽  
Anti Inflammatory

To sdudy the synthesis and biological activities of 1,2,4-triazine derivatives, a series of 1,2,4-triazines were prepared from the reaction of 3-mercapto-5-hydroxyl-6-methyl-1,2,4-triazine with alkyl halide.The structures of prepared compounds were confirmed by IR,1H-NMR and elemental analysis. Biological activities showed the compounds had anti-inflammatory activities.

scholarly journals Synthesis and Anti-inflammatory Activity of Some Novel 3-(6-Substituted-1, 3-benzothiazole-2-yl)-2-[{(4-substituted phenyl) amino} methyl] quinazolines-4 (3H)-ones

2009 ◽  
Vol 6 (4) ◽  
pp. 1055-1062 ◽  
Author(s):  
Manish Srivastav ◽  
MD. Salahuddin ◽  
S. M. Shantakumar
Keyword(s):  
Antibacterial Activity ◽  
Benzoic Acid ◽  
Spectral Data ◽  
Elemental Analysis ◽  
Inflammatory Activity ◽  
Mass Spectral Data ◽  
Mass Spectral ◽  
Anti Inflammatory ◽  
Substituted 1 ◽  
Amino Benzoic Acid

A series of novel 3-(6-substituted-1, 3-benzothiazole-2-yl)-2-[{(4-substituted phenyl) amino} methyl] quinazolines-4(3H)-ones were synthesized by treating 2-(chloromethyl)-3-(6-substituted-1, 3-benzothiazole-2-yl) quinazoline-4-(3H)-one (IIa-d) with various substituted amine. The compounds (IIa-d) prepared by treating 2-[(chloroacetyl) amino] benzoic acid with different 2-amino-6-substituted benzothiazole. Elemental analysis, IR,1HNMR and mass spectral data confirmed the structure of the newly synthesized compounds. Synthesized quinazolines-4-one derivative were investigated for their anti-inflammatory and antibacterial activity.

scholarly journals Anti-Inflammatory Activity of Dried Ginger Mediated Iron Nanoparticles

2020 ◽  
pp. 14-19
Author(s):  
Sai Sree Lasya Ganta ◽  
M. Jeevitha ◽  
S. Preetha ◽  
S. Rajeshkumar
Keyword(s):  
Iron Nanoparticles ◽  
Size Range ◽  
Catalytic Properties ◽  
Inflammatory Diseases ◽  
Biological Activities ◽  
Inflammatory Activity ◽  
Inflammatory Agent ◽  
Vis Spectroscopy ◽  
Anti Inflammatory ◽  
Inflammatory Effect

Nanotechnology is a branch of science and technology relating to the matter on the atomic and molecular scale in the size range between 1-100 nm. Iron nanoparticles have diverse diagnostic and potential therapeutic applications with unique magnetic and catalytic properties and potent biological activities. The present study aimed to analyse the anti-inflammatory activity of iron nanoparticles synthesized from dried ginger. The synthesized iron nanoparticles were characterized using UV-vis spectroscopy and evaluated for anti-inflammatory activity by inhibition of albumin denaturation assay. The nanoparticles showed maximum absorbance at 360 nm and revealed potent anti-inflammatory effect with maximum of 83.5% inhibition at lowest concentration of 50 µl and thus can be used as an anti-inflammatory agent in various inflammatory diseases.

scholarly journals Profile of Similarity of Electron Withdrawing Structure Towards Analgesic-Anti-Inflammatory Activity of The Novel Isatin Analogue: Design and Implementation of Phase I Drug Discovery

2018 ◽  
pp. 7-14
Author(s):  
Rahul Hajare
Keyword(s):  
Drug Discovery ◽  
Phase I ◽  
Biological Activities ◽  
Mannich Bases ◽  
Inflammatory Activity ◽  
Spectral Studies ◽  
The Novel ◽  
Schiff’S Bases ◽  
Design And Implementation ◽  
Anti Inflammatory

Isatin (1H-indole-2,3-dione ) and derivatives demonstrate a diverse array of biological activities. Isatin and 5-halo derivatives has reacted to form the schiff’s bases , mannich bases and friedal craft alkylation’s to form C-C, C-N, C=N bonds. From the spectral studies, isatin has undergoes reaction at C-3 and N-1 position and synthesized lead in present schme and seen the similarity of structure and analgesic-anti-inflammatory activity.

scholarly journals Synthesis, Characterization, and Anti-Inflammatory Activity of Newer Quinazolinone Analogs

2013 ◽  
Vol 2013 ◽  
pp. 1-7 ◽  
Author(s):  
Chatrasal Singh Rajput ◽  
Shiwani Singhal
Keyword(s):  
Spectral Data ◽  
Elemental Analysis ◽  
Inflammatory Activity ◽  
Mass Spectral Data ◽  
Mass Spectral ◽  
Anti Inflammatory ◽  
Analgesic Activities

A series of 3-[2′-(Substitutedbenzylideneamino)phenyl]-2-methyl-6-substituted quinazolin-4-ones (5–10), 3-[2′-(3″-chloro-2″-oxo-4″-substitutedphenylazetidin-1″-yl)phenyl]-2-methyl-6-substitutedquinazolin-4-ones (11–16), and 3-[2′-(2″-substitutedphenyl-4″-oxo-1″,3″-thiazolidin-3″-yl)phentl]-2-methyl-6-substitutedquinazolin-4-ones (17–22) have been synthesized in the present study. The structures of the synthesized compounds were assigned on the basis of elemental analysis, IR, H1 NMR, and mass spectral data. All the newly synthesized compounds were screened for anti-inflammatory and analgesic activities.

Facile Synthesis, Characterization and Anti-Inflammatory Effect of 3-Aminoindolizine Derivatives

2014 ◽  
Vol 881-883 ◽  
pp. 446-449
Author(s):  
Yong Wei ◽  
Cheng Qiao Cao ◽  
Xiao Feng Lu ◽  
Zheng Yang ◽  
Kun Zou ◽  
...  
Keyword(s):  
Elemental Analysis ◽  
Biological Activities ◽  
Bacterial Lipopolysaccharide ◽  
Facile Synthesis ◽  
Inflammation Model ◽  
Mouse Cells ◽  
Inflammatory Drugs ◽  
Anti Inflammatory ◽  
Stimulation Of ◽  
Inflammatory Effect

Four 3-aminoindolizines were synthesized from the substituted 2-bromopyridines and propargyl amines with the aim of obtaining potential anti-inflammatory compounds, which were characterized by NMR, IR, ESI-MS and elemental analysis. Their biological activities were evaluated by the bacterial lipopolysaccharide (LPS) stimulation of mouse cells in the RAW264.7 inflammation model. The target compounds4a-4drevealed moderate anti-inflammatory effects with the inhibitions of 45%~61% at 50 μM. The bioactive 3-aminoindolizines might be used for further optimization as potential anti-inflammatory drugs.

Design, Synthesis, Characterization and in silico molecular docking studies and in vivo anti-inflammatory Activity of Pyrazoline clubbed Thiazolinone Derivatives

2020 ◽  
Vol 17 ◽  
Author(s):  
Deepak Kumar Singh ◽  
Mayank Kulshreshtha ◽  
Yogesh Kumar ◽  
Pooja A Chawla ◽  
Akash Ved ◽  
...  
Keyword(s):  
Molecular Docking ◽  
Biological Activities ◽  
Inflammatory Activity ◽  
Standard Drug ◽  
Docking Score ◽  
Chemical Structures ◽  
Cox 2 ◽  
Anti Inflammatory ◽  
Cox 1

Background: The pyrazolines give the reactions of aliphatic derivatives, resembling unsaturated compounds in their behavior towards permanganate and nascent hydrogen. This nucleus has been associated with various biological activities including inflammatory. Thiazolinone is a heterocyclic compound that contains both sulfur and nitrogen atom with a carbonyl group in their structure.Thiazolinone and their derivatives have attracted continuing interest because of their various biological activities, such as anti-inflammatory, antimicrobial, anti-proliferative, antiviral, anticonvulsant etc. The aim of the research was to club pyrazoline nucleus with thiazolinone in order to have significantanti-inflammatory activity. The synthesized compounds were chemically characterized for the establishment of their chemical structures and to evaluate as anti-inflammatory agent. Method: In the present work, eight derivatives of substituted pyrazoline (PT1-PT8) were synthesized by a three step reaction.The compounds were subjected to spectral analysis by Infrared, Mass and Nuclear magnetic resonance spectroscopy and elemental analysis data. All the synthesized were evaluated for their in vivo anti-inflammatory activity. The synthesized derivatives were evaluated for their affinity towards target COX-1 and COX-2, using indomethacin as the reference compound molecular docking visualization through AutoDock Vina. Results: Compounds PT-1, PT-3, PT-4 and PT-8 exhibited significant anti-inflammatory activity at 3rd hour being 50.7%, 54.3%, 52.3% and 57% respectively closer to that of the standard drug indomethacin (61.9%).From selected anti-inflammatory targets, the synthesized derivatives exhibited better interaction with COX-1 and COX-2 receptor, where indomethacin showed docking score of -6.5 kJ/mol, compound PT-1 exhibited highest docking score of -9.1 kJ/mol for COX-1 and compound PT-8 having docking score of 9.4 kJ/mol for COX-2. Conclusion: It was concluded that synthesized derivatives have more interaction with COX-2 receptors in comparison to the COX-1 receptors because the docking score with COX-2 receptors were very good. It is concluded that the synthesized derivatives (PT-1 to PT-8) are potent COX-2 inhibitors.

scholarly journals Biosynthesis of resveratrol derivatives and evaluation of their anti-inflammatory activity

2021 ◽  
Vol 64 (1) ◽  
Author(s):  
Yoojin Chong ◽  
Hye Lim Lee ◽  
Jihyeon Song ◽  
Youngshim Lee ◽  
Bong-Gyu Kim ◽  
...  
Keyword(s):  
Biological Activities ◽  
Stilbene Synthase ◽  
Inflammatory Activity ◽  
E Coli ◽  
Prephenate Dehydrogenase ◽  
Coa Ligase ◽  
Final Yield ◽  
Resveratrol Derivatives ◽  
Anti Inflammatory ◽  
Tyrosine Biosynthesis

AbstractResveratrol is a typical plant phenolic compound whose derivatives are synthesized through hydroxylation, O-methylation, prenylation, and oligomerization. Resveratrol and its derivatives exhibit anti-neurodegenerative, anti-rheumatoid, and anti-inflammatory effects. Owing to the diverse biological activities of these compounds and their importance in human health, this study attempted to synthesize five resveratrol derivatives (isorhapontigenin, pterostilbene, 4-methoxyresveratrol, piceatannol, and rhapontigenin) using Escherichia coli. Two-culture system was used to improve the final yield of resveratrol derivatives. Resveratrol was synthesized in the first E. coli cell that harbored genes for resveratrol biosynthesis including TAL (tyrosine ammonia lyase), 4CL (4-coumaroyl CoA ligase), STS (stilbene synthase) and genes for tyrosine biosynthesis such as aroG (deoxyphosphoheptonate aldolase) and tyrA (prephenate dehydrogenase). Thereafter, culture filtrate from the first cell was used for the modification reaction carried out using the second E. coli harboring hydroxylase and/or O-methyltransferase. Approximately, 89.8 mg/L of resveratrol was synthesized and using the same, five derivatives were prepared with a conversion rate of 88.2% to 22.9%. Using these synthesized resveratrol derivatives, we evaluated their anti-inflammatory activity. 4-Methoxyresveratrol, pterostilbene and isorhapontigenin showed the anti-inflammatory effects without any toxicity. In addition, pterostilbene exhibited the enhanced anti-inflammatory effects for macrophages compared to resveratrol.

AN UPDATE ON THE SYNTHESIS OF BENZOXAZOLES

2017 ◽  
Vol 10 (10) ◽  
pp. 48 ◽  
Author(s):  
Jyothi M ◽  
Ramchander Merugu
Keyword(s):  
Central Nervous System ◽  
Nervous System ◽  
Biological Activity ◽  
Biological Activities ◽  
Starting Material ◽  
Bioactive Molecules ◽  
Living Systems ◽  
Inflammatory Activity ◽  
Anti Inflammatory

Benzoxazoles being structurally similar to bases adenine and guanine interact with biomolecules present in living systems. These compounds possess antimicrobial, central nervous system activities, antihyperglycemic potentiating activity, analgesic, and anti-inflammatory activity. It can also be used as starting material for other bioactive molecules. Modifications in structure and the biological profiles of new generations of benzoxazoles were found to be more potent with enhanced biological activity. Considering all these, we have prepared this review and discussed the synthesis and biological activities of benzoxazoles.

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