A rapid solid supported synthesis of 4-amino-5-(pyridin-4-YL)-4H-1,2,4-triazol-3-thiol and its derivatives

2019 ◽  
Author(s):  
Chem Int
Keyword(s):  
Solid State ◽  
Microwave Irradiation ◽  
Future Study ◽  
Biological Activities ◽  
Uv Visible ◽  
Anti Inflammatory ◽  
Derivatives Of

1,2,4-triazoles and its substituted derivatives were synthesized since these compounds are known for their excellent antibacterial, antifungal, anti-tubercular, antioxidant, anticancer, anti-inflammatory, analgesic, anticonvulsant and anxiolytic activities. 1,2,4-triazole and substituted derivatives of 1,2,4-triazole were synthesized using solid state microwave irradiation technique and synthesized compounds were characterized by UV-Visible, FTIR and GC-MS techniques and in future study the biological activities of synthesized compounds will be studied.

scholarly journals PYRIMIDINES AS POTENT CYTOTOXIC AND ANTI-INFLAMMATORY AGENTS

2017 ◽  
Vol 10 (6) ◽  
pp. 237 ◽  
Author(s):  
Ishwar Bhat K ◽  
Abhishek Kumar
Keyword(s):  
Acetic Acid ◽  
Cytotoxic Activity ◽  
Glacial Acetic Acid ◽  
Antimalarial Activity ◽  
Biological Activities ◽  
Cytotoxic Agents ◽  
Pyrimidine Derivatives ◽  
Pharmacological Activities ◽  
Anti Inflammatory ◽  
Derivatives Of

Objective: Many derivatives of pyrimidine are known for the broad-spectrum biological activities such as antimicrobial, antitumor, antibacterial, antitubercular, anti-inflammatory, and cytotoxic activity. Chalcones with an enone group show potent pharmacological activities such as antiinflammatory, antibacterial, antifungal, and antimalarial activity. A series of pyrimidines from chalcones have been synthesized and screened for anti-inflammatory and cytotoxic activity studies.Methods: Chalcones [1-(4-nitrophenyl)-3-substituted-phenylprop-2-en-1-one] were synthesized from various substituted aldehydes with 4-nitroacetophenone and cyclized with urea and glacial acetic acid to give pyrimidine derivatives [4-(4-nitrophenyl)-6-substituted-phenylpyrimidin-2-ol].Results: Anti-inflammatory and cytotoxic activity studies revealed that some of the synthesized compounds have shown significant activity.Conclusion: The observed results proved that pyrimidines are found to be interesting lead molecules for the synthesis of anti-inflammatory and cytotoxic agents

scholarly journals UJI AKTIVITAS ANTIOKSIDAN SENYAWA PIRAZOLIN 3-(2- METOKSI-FENIL)-5-NAFTALEN-1-IL-4,5-DIHIDRO-1H-PIRAZOL

2018 ◽  
Vol 8 (2) ◽  
pp. 53-58
Author(s):  
Nurlaili ◽  
Jasril ◽  
Hilwan Yuda Teruna
Keyword(s):  
Antioxidant Activity ◽  
Acetic Acid ◽  
Microwave Irradiation ◽  
Biological Activities ◽  
Spectroscopy Data ◽  
Activity Test ◽  
Ic50 Value ◽  
Dpph Method ◽  
Anti Inflammatory

Pyrazoline compounds are reported to have many useful biological activities such as antimicrobials, antihyperglycemia, antioxidants, anti-inflammatory, anticancer and anticonvulsants. The pyrazoline analogues of 3- (2-methoxy-phenyl) -5-naphthalene-1-yl-4,5-dihydro-1H-pyrazol were synthesized usingglacial acetic acid as catalyst and assisted by microwave irradiation. The structures of the compounds were obtainedby UV, IR and HRMS spectroscopy data. Antioxidant activity test using DPPH method showed that pyrazoline compound had IC50 value of 27.41 μg/mL.

scholarly journals Resveratrol Oligomers for the Prevention and Treatment of Cancers

2014 ◽  
Vol 2014 ◽  
pp. 1-9 ◽  
Author(s):  
You-Qiu Xue ◽  
Jin-Ming Di ◽  
Yun Luo ◽  
Ke-Jun Cheng ◽  
Xing Wei ◽  
...  
Keyword(s):  
Research And Development ◽  
Human Health ◽  
Drug Research ◽  
Biological Activities ◽  
Anticancer Properties ◽  
Prevention And Treatment ◽  
Significant Interest ◽  
Anti Inflammatory ◽  
Derivatives Of

Resveratrol (3,4′,5-trihydroxystilbene) is a naturally derived phytoalexin stilbene isolated from grapes and other plants, playing an important role in human health and is well known for its extensive bioactivities, such as antioxidation, anti-inflammatory, anticancer. In addition to resveratrol, scientists also pay attention to resveratrol oligomers, derivatives of resveratrol, which are characterized by the polymerization of two to eight, or even more resveratrol units, and are the largest group of oligomeric stilbenes. Resveratrol oligomers have multiple beneficial properties, of which some are superior in activity, stability, and selectivity compared with resveratrol. The complicated structures and diverse biological activities are of significant interest for drug research and development and may provide promising prospects as cancer preventive and therapeutical agents. This review presents an overview on preventive or anticancer properties of resveratrol oligomers.

The exhaustive reduction of formylporphyrins to methylporphyrins using dimethylformamide/water as reductant under microwave irradiation

2014 ◽  
Vol 18 (03) ◽  
pp. 200-208 ◽  
Author(s):  
Sarah J. Fletcher ◽  
Shannon R. Harper ◽  
Dennis P. Arnold
Keyword(s):  
Microwave Irradiation ◽  
Microwave Heating ◽  
Trifluoroacetic Acid ◽  
High Yield ◽  
Primary Alcohols ◽  
Visible Spectra ◽  
Added Water ◽  
Methyl Derivatives ◽  
Uv Visible ◽  
Derivatives Of

The reduction of meso-formyl derivatives of 5,15-diaryl- and 5,10,15-triphenylporphyrin (and their nickel(II) complexes) to the corresponding meso-methyl porphyrins is achieved in high yield by microwave heating of the substrate in dimethylformamide (DMF) in the presence of acids such as trifluoroacetic acid, or even just with added water. The reactions are complete in less than 30 min at 250 °C. The reaction is strongly suppressed in very dry DMF in the absence of added acid. The meso-hydroxymethyl porphyrins are also reduced to the methyl derivatives, suggesting the primary alcohols may be intermediates in the exhaustive reduction. UV-visible spectra taken at intervals during reaction at 240 °C indicated that at least one other intermediate is present, but it was not identified. In d7-DMF, the methylporphyrin isolated was mainly Por-CD2H, showing that both of the added hydrogens arise from the solvent, and not from the added water or acid.

scholarly journals COUMARINS: A UNIQUE SCAFFOLD WITH VERSATILE BIOLOGICAL BEHAVIOR

2019 ◽  
pp. 27-38 ◽  
Author(s):  
MANDEEP KUMAR GUPTA ◽  
SUSHIL KUMAR ◽  
SACHIN CHAUDHARY
Keyword(s):  
Pharmacological Activity ◽  
Biological Activities ◽  
Biological Behavior ◽  
Pharmacokinetic Studies ◽  
Coumarin Derivatives ◽  
Toxicological Studies ◽  
Anti Inflammatory ◽  
Derivatives Of ◽  
Anti Hiv

Benzopyrones are the club of compounds that can be coumarins or flavonoids. The hydroxyl derivatives of coumarins such as 4-hydroxycoumarins and 7-hydroxycoumarins have extensive biological activities which have employed for the synthesis of miscellaneous coumarin derivatives. These derivatives have exhibited impressive pharmacological and physiological activities such as anticoagulant, antibacterial, antiviral, antitumor, bactericidal, fungicidal, anti-inflammatory agents, and anti-HIV activity. This review comprised pharmacokinetic studies, including absorption, distribution, and metabolism of coumarin analogs along with toxicological studies. The studies of coumarins and their derivatives exhibiting immense pharmacological activity are also summarized in the current study.

scholarly journals Review Article: Various Biological Activities of Coumarin and Oxadiazole Derivatives.

2017 ◽  
Vol 10 (7) ◽  
pp. 38 ◽  
Author(s):  
Sunny Jalhan
Keyword(s):  
Biological Activities ◽  
Biochemical Properties ◽  
Review Article ◽  
Pharmacological Activities ◽  
Wide Range ◽  
Methylene Groups ◽  
Anti Oxidant ◽  
Oxadiazole Derivatives ◽  
Anti Inflammatory ◽  
Derivatives Of

In this review article data is collected regarding the various derivatives of coumarin and oxadiazole as both these have wide range of biological activities and they can be further modified to synthesize more effective and potent drugs. Coumarin class of organic compounds consists of 1,2-benzopyrone ring system as a basic parent scaffold. These benzopyrones are subdivided into alpha-benzopyrones and gamma benzopyrones; with coumarin class of compounds belonging to alpha-benzopyrones. Since the last few years, coumarins were synthesized in many of their derivative forms. Their pharmacological, therapeutic and biochemical properties depend upon their pattern of substitution. Coumarins exhibit a wide range of pharmacological activities, which includes anti-diabetic, anti-viral, anti-microbial, anticancer, anti-oxidant, anti-parasitic, anti-helminthic, anti-proliferative, anti-convulsant, anti-inflammatory and antihypertensive activities. 1,3,4-Oxadiazole is a heterocyclic compound containing an oxygen atom and two nitrogen atoms in a five-membered ring. It is derived from furan by substitution of two methylene groups (=CH) with two pyridine type nitrogens (-N=). There are three known isomers: 1,2,4-oxadiazole, 1,2,3-oxadiazole and 1,2,5- oxadiazole. Oxadiazole moiety shows antimicrobial, anticancer and anti-inflammatory activity and suitably substituted 1,3,4-oxadiazole having biological activities like antimicrobial, anticancer and other biological activities.

scholarly journals 3,4-dihydro-2H-1,3-benzoxazines and their oxo-derivatives chemistry and bioactivities

2020 ◽  
pp. 1-1 ◽  
Author(s):  
El-Din Sharaf
Keyword(s):  
Biological Activity ◽  
Bioactive Compounds ◽  
Biological Activities ◽  
Anti Inflammatory ◽  
Derivatives Of ◽  
Anti Hiv ◽  
Significant Class

3,4-Dihydro-2H-1,3-benzoxazines derivatives are a significant class of heterocycles with a particular awareness due to their remarkable biological activities in humans, plant as well as in animals and also, they are naturally occurrence. Because of alteration in the benzoxazines skeleton, beside their comparative chemical simplicity and accessibility, make these compounds to be suitable sources of other bioactive compounds. Resulting in the discovery of a wide set of these compounds that have a broad biological activity such as antifungal, antibacterial, anti-HIV, anticancer, anticonvulsant, anti-inflammatory and so on. Subsequently, this review herein gives a brief overview of derivatives of 3,4-dihydro-2H-1,3-benzoxazines monomers and their oxo-derivatives chemistry and bioactivities.

scholarly journals Studying of analgesic and anti-inflammatory activity of 2,4-dioxobutanoic acid hydrazine derivatives

2020 ◽  
Vol 37 (4) ◽  
pp. 115-119
Author(s):  
Natalia A. Pulina ◽  
Aleksander S. Kuznecov ◽  
Svetlana V. Chashchina
Keyword(s):  
Biological Activities ◽  
Biological Effects ◽  
Water Soluble ◽  
Inflammatory Activity ◽  
Synthesis Methods ◽  
Hot Plate Test ◽  
Hydrazine Derivatives ◽  
Anti Inflammatory ◽  
The Relationship ◽  
Derivatives Of

Objective. To study the analgesic and anti-inflammatory activity of water-soluble hydrazine derivatives of 2,4-dioxobutanoic acids, as well as to determine the relationship between the structure of substances and their biological effects. Materials and methods. The laboratory synthesis methods were applied to obtain 2-hydrazine derivatives of 2,4-dioxobutanoic acids. The compounds were tested for biological activity using a hot plate test in mice and an acute inflammatory reaction caused by carrageenan-induced paw edema in rats. Results. The analgesic activity of four compounds is comparable to that of nimesulide. One of the substances obtained is found to exhibit higher anti-inflammatory activity than nimesulide during the 1st and 3rd hours of the experiment. Two compounds with a combination of high analgesic and anti-inflammatory activity were identified. The effect of certain radicals in the structure of the substances on the activities studied was discovered. Conclusions. The revealed relationship between the structure of original compounds and their biological activities can be used in the further synthesis and search for new domestic pharmaceutical substances with investigated effects.

scholarly journals Microbial Transformation of Prenylquercetins by Mucor hiemalis

Molecules ◽  
2020 ◽  
Vol 25 (3) ◽  
pp. 528 ◽  
Author(s):  
Fubo Han ◽  
Yina Xiao ◽  
Ik-Soo Lee
Keyword(s):  
Water Solubility ◽  
Biological Activities ◽  
Microbial Transformation ◽  
Mass Spectrometric ◽  
Microbial Metabolites ◽  
Mucor Hiemalis ◽  
Chemical Structures ◽  
Polar Metabolites ◽  
Anti Inflammatory ◽  
Derivatives Of

Quercetin, one of the most widely distributed flavonoids, has been found to show various biological activities including antioxidant, anticancer, and anti-inflammatory effects. It has been reported that bioactivity enhancement of flavonoids has often been closely associated with nuclear prenylation, as shown in 8-prenylquercetin and 5′-prenylquercetin. It has also been revealed in many studies that the biological activities of flavonoids could be improved after glucosylation. Three prenylated quercetins were prepared in this study, and microbial transformation was carried out in order to identify derivatives of prenylquercetins with increased water solubility and improved bioavailability. The fungus M. hiemalis was proved to be capable of converting prenylquercetins into more polar metabolites and was selected for preparative fermentation. Six novel glucosylated metabolites were obtained and their chemical structures were elucidated by NMR and mass spectrometric analyses. All the microbial metabolites showed improvement in water solubility.

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