scholarly journals Design and Microwave Assisted Synthesis of Coumarin Derivatives as PDE Inhibitors

2016 ◽  
Vol 2016 ◽  
pp. 1-16 ◽  
Author(s):  
Mahadev N. Kumbar ◽  
Ravindra R. Kamble ◽  
Atulkumar A. Kamble ◽  
Sujith Raj Salian ◽  
Sandhya Kumari ◽  
...  

Coumarins appended to benzimidazole through pyrazole are designed and synthesized using microwave irradiation. These compounds were analyzed for phosphodiesterase (PDE) inhibition indirectly by motility pattern in human spermatozoa. Some of the synthesized compounds, namely, 5d, 5e, 5f, 5g, 5h, and 5k, have exhibited potent inhibitory activity on PDE.

2020 ◽  
Vol 7 (3) ◽  
pp. 183-195
Author(s):  
Musa Özil ◽  
Emre Menteşe

Background: Benzoxazole, containing a 1,3-oxazole system fused with a benzene ring, has a profound effect on medicinal chemistry research owing to its important pharmacological activities. On the other hand, the benzoxazole derivative has exhibited important properties in material science. Especially in recent years, microwave-assisted synthesis is a technique that can be used to increase diversity and quick research in modern chemistry. The utilization of microwave irradiation is beneficial for the synthesis of benzoxazole in recent years. In this focused review, we provide a metaanalysis of studies on benzoxazole in different reaction conditions, catalysts, and starting materials by microwave technique so far, which is different from conventional heating. Methods: Synthesis of different kind of benzoxazole derivatives have been carried out by microwave irradiation. The most used method to obtain benzoxazoles is the condensation of 2-aminophenol or its derivatives with aldehydes, carboxylic acids, nitriles, isocyanates, and aliphatic amines. Results: Benzoxazole system and its derivatives have exhibited a broad range of pharmacological properties. Thus, many scientists have remarked on the importance of the synthesis of different benzoxazole derivatives. Conventional heating is a relatively inefficient and slow method to convey energy in orientation to the reaction medium. However, the microwave-assisted heating technique is a more effective interior heating by straight coupling of microwave energy with the molecules. Conclusion: In this review, different studies were presented on the recent details accessible in the microwave- assisted techniques on the synthesis of the benzoxazole ring. It presents all examples of such compounds that have been reported from 1996 to the present. Benzoxazoles showed an extensive class of chemical substances not only in pharmaceutical chemistry but also in dyestuff, polymer industries, agrochemical, and optical brighteners. Thus the development of fast and efficient achievement of benzoxazoles with a diversity of substituents in high yield is getting more noteworthy. As shown in this review, microwave-assisted synthesis of benzoxazoles is a very effective and useful technique.


2005 ◽  
Vol 2005 (1) ◽  
pp. 27-28 ◽  
Author(s):  
Jaime Charris ◽  
Arthur Barazarte ◽  
José Domínguez ◽  
Neira Gamboa

A rapid method for the preparation of N-aryl-2-methylthio-4-oxo-1,4-dihydro quinoline-3-carbonitriles (2a–e) and N-aryl-3-methylthio-4H-1,4-benzothiazine-2-carbonitrile 1,1-dioxides (2f–o) is reported. The cyclization is accelerated by microwave irradiation under solvent free conditions in the presence of K2CO3.


Author(s):  
Mousumi Chakraborty ◽  
Sanjay Baweja ◽  
Sunita Bhagat ◽  
TejpalSingh Chundawat

Abstract In the present study Schiff’s bases are synthesized by the conventional as well as by microwave irradiation. Excellent yield within short reaction time is obtained using microwave irradiation along with other advantages like mild reaction condition, non-hazardous and safer environmental conditions. The effects of temperature, reactant molar ratio, and microwave power variation on yield are observed. Mathematical model has been developed using matlab software to obtain the yield as a function of microwave power. Kinetic study of the reaction has also been attempted. Schiff’s bases structures are confirmed by IR, 1HNMR, Mass Spectra and elemental analysis.


Molecules ◽  
2020 ◽  
Vol 25 (6) ◽  
pp. 1467
Author(s):  
Rafaela Teixeira ◽  
Talita Menengat ◽  
Gabriel Andrade ◽  
Bruno Cotrim ◽  
Cristiano Ponte ◽  
...  

Quinazolinones have pharmacological effects on vascular reactivity through different mechanisms. We synthesized 4-phenylquinazolin-2(1H)-one derivatives under microwave irradiation and tested them on the rat thoracic aorta. The prepared compounds 2a–2f were obtained in about 1 h with suitable yields (31–92%). All derivatives produced vasorelaxant effects with IC50 values ranging from 3.41 ± 0.65 µM to 39.72 ± 6.77 µM. Compounds 2c, 2e and 2f demonstrated the highest potency in endothelium-intact aorta rings (IC50 4.31 ± 0.90 µM, 4.94 ± 1.21 µM and 3.41 ± 0.65 µM respectively), and they achieved around 90% relaxation (30 μM). In aorta rings without an endothelium, the effect of compound 2f was abolished. Using the MTT assay to test for cell viability, only compound 2b induced cytotoxicity at the maximum concentration employed (30 µM). The results show that vasorelaxation by 4-phenylquinazolin-2(1H)-one derivatives might depend on the activation of a signalling pathway triggered by endothelium-derived factors.


2020 ◽  
Vol 49 (14) ◽  
pp. 4518-4527 ◽  
Author(s):  
José Miranda de Carvalho ◽  
David Van der Heggen ◽  
Lisa I. D. J. Martin ◽  
Philippe F. Smet

Microwave irradiation leads to highly homogeneous emitting sites, and large storage capacity in persistent luminescence materials after the reducing step.


2019 ◽  
Vol 31 (5) ◽  
pp. 993-996 ◽  
Author(s):  
Sanjay S. Kotalwar ◽  
Amol D. Kale ◽  
Ram B. Kohire ◽  
Vasant B. Jagrut

An efficient and eco-friendly synthesis of 1,5-benzothiazepines has been developed by the reaction of various 2-propen-1-ones with 2-aminothiophenol using microwave irradiation in greener reaction medium, glycerol. The clean reaction conditions, shorter reaction time, high yields and non-toxic, biodegradable reaction medium manufactured from renewable sources are unique features of this method.


2018 ◽  
Vol 24 (3) ◽  
pp. 125-128 ◽  
Author(s):  
Massimiliano Lamberto

Abstractγ-Thiolactams were synthesized in good yields from ethyl isocyanoacetate through a sequential alkylation/isothiocyanation/radical cyclization under microwave irradiation.


2005 ◽  
Vol 2005 (1) ◽  
pp. 71-72 ◽  
Author(s):  
Xi-Cun Wang ◽  
Zheng-Jun Quan ◽  
Zheng Li

Thirty-two 1-aroyl/aryloxyacetyl-4-(2-furoyl)thiosemicarbazides and corresponding semicarbazides were synthesised in excellent yields under microwave irradiation and solvent-free conditions without using any catalyst.


RSC Advances ◽  
2015 ◽  
Vol 5 (124) ◽  
pp. 102682-102688 ◽  
Author(s):  
Ming Hong ◽  
Tongtong Xuan ◽  
Jiaqing Liu ◽  
Ziyao Jiang ◽  
Yiwei Chen ◽  
...  

CIS/ZnS QDs were synthesized by microwave irradiation in air. The fabricated QDs/PMMA composite films were first applied to Si solar cells to improve the conversion efficiency by 3.8%.


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