One-Pot Multicomponent Synthesis of Novel 2-Tosyloxyphenylpyrans under Green and Conventional Condition with Anti-inflammatory Activity

2016 ◽  
Vol 54 (2) ◽  
pp. 1442-1449 ◽  
Author(s):  
Ahmed Khodairy ◽  
Ali M. Ali ◽  
Moustafa O. Aboelez ◽  
M. T. El-Wassimy
2019 ◽  
Vol 21 ◽  
pp. 100233 ◽  
Author(s):  
Kiran N. Patil ◽  
Rohan A. Mane ◽  
Sandip B. Jadhav ◽  
Mansing M. Mane ◽  
Vasant B. Helavi

2020 ◽  
Vol 16 (8) ◽  
pp. 1161-1165
Author(s):  
Bashetti Nagaraju ◽  
Jagarlapudi V. Shanmukhakumar ◽  
Nareshvarma Seelam ◽  
Tondepu Subbaiah ◽  
Bethanamudi Prasanna

Background: Recently, there has been a lot of scientific interest in exploring the syntheses of oxygen and nitrogen-containing heterocyclic compounds due to their pharmacological activities. In addition, benzisoxazoles play a very important role in organic synthesis as key intermediates. Objective: In this paper, we focused on developing a novel synthetic route for biologically active arylisoxazoles under normal conditions, and simplified it to get high purities and yields, and also reported their anti-inflammatory activities. Method: An efficient and simple method has been explored for the synthesis of novel 3-methyl arylisoxazoles from o-nitroaryl halides via o-ethoxyvinylnitroaryls, using dihydrated stannous chloride (SnCl2.2H2O) in MeOH / EtOAc (1:1) via Domino rearrangement in one pot synthesis. Result: We synthesized novel 3-methylarylisoxazoles from o-nitroarylhalides via o-ethoxyvinylnitroaryls, using dihydrated stannous chloride (SnCl2.2H2O) in MeOH / EtOAc (1:1) via domino rearrangement. In this reduction, nitro group and ethoxy vinyl group change to the functional acyl ketones, followed by hetero cyclization. Here, the reaction proceeds without the isolation of intermediates like 2-acylnitroarenes and 2- acylanilines. All the synthesized compounds were completely characterized by the NMR and mass spectra. The compounds were also explored for their anti-inflammatory activity by carrageenan-induced inflammation in the albino rats (150-200 g) of either sex used in this entire study with the use of Diclofenac sodium as the standard drug. The initial evaluations identified leading targets with good to moderate anti-inflammatory activity. Conclusion: A simple, one-pot and convenient method has been explored for the synthesis of novel 3- methylarylisoxazoles with high purity and reaction yields. All the compounds 3a, 3c, 3d, 3f, 3g and 3h exhibited 51-64% anti-inflammatory activities.


2018 ◽  
Vol 30 (2) ◽  
pp. 403-410 ◽  
Author(s):  
Venkata Swamy Tangeti ◽  
Boyi Harika Reddy ◽  
K. Sharon Evangeline

2019 ◽  
Vol 4 (1) ◽  
pp. 14-19
Author(s):  
B. Sujatha ◽  
P. Kamala

In the present report, an expeditious green synthetic approach was developed for the synthesis of α-aminophosphonates 5(a-j) in good yields through one-pot three component reaction (Kabachnik-Fields reaction) in solvent-free conditions under microwave irradiation. The newly synthesized compounds were characterized by IR, NMR (1H, 13C and 31P), mass and C, H, N analysis. The synthesized compounds were screened for their anti-inflammatory activity using rat paw edema method. Most of the compounds from the series showed significant (p < 0.05) anti-inflammatory activity.


2019 ◽  
Vol 49 (20) ◽  
pp. 2725-2759 ◽  
Author(s):  
Prateek Pathak ◽  
Parjanya Kumar Shukla ◽  
Vladislav Naumovich ◽  
Maria Grishina ◽  
Vladimir Potemkin ◽  
...  

A novel series of a hybrid class of hybrid thiazolidin-4-one derivatives were designed and synthesized through one-pot catalytic synthesis. The reaction was catalyzed in the presence of silica-H2SO4(+6). The derivatives computational ADMET profile was calculated. The study shows that most active derivatives have optimal logP, higher anti-inflammatory activity score, and poor metabolism at the sight of P450-3A4 and 2D6. The entire series of derivatives were further evaluated for anti-tubercular (against Mycobacterium tuberculosis H37Rv (Resistant strain)) and anti-inflammatory activity (in-vivo assay using Wistar rat). The result showed that derivatives 4c, 4h, and 4m have significant potency against tested M. tuberculosis. However, derivatives 4i and 4j found significantly active against inflammation. In vitro COX inhibition assay also supported the result in favor of selectivity and efficacy of derivatives.


2016 ◽  
Vol 26 (3) ◽  
pp. 858-863 ◽  
Author(s):  
Yasodakrishna Sajja ◽  
Hanmanth Reddy Vulupala ◽  
Rajashaker Bantu ◽  
Lingaiah Nagarapu ◽  
Sathish Babu Vasamsetti ◽  
...  

Author(s):  
Sudharshan Reddy Sudula ◽  
Ranjith Jala ◽  
Kavitha Siddoju ◽  
Jagadeesh Kumar Ega

2021 ◽  
Vol 38 ◽  
pp. 127860
Author(s):  
Alejandra Chávez-Riveros ◽  
Eduardo Hernández-Vázquez ◽  
Ángel Ramírez-Trinidad ◽  
Antonio Nieto-Camacho ◽  
Luis D. Miranda

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