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Novel [1,2,4]triazolo[4,3-c]pyrimidine-8-carboxamides were synthesized via oxidative cyclization of hydrazono-1,6-dihydropyrimidine-5-carboxamide intermediates by the application of iodobenzenediacetate as a sole cyclizing agent. Here, we report a one-pot sequential strategy to generate the corresponding triazolopyrimidines by condensation of preprepared α-acylketene dithioacetals and arylamidines. Moreover, this process describes the application of presynthesized arylamidines, which omits the Suzuki–Miyaura cross-coupling reaction and hence provides metal-free organic synthesis in an atom- and step-economical fashion. 相似文献
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Jignasa Savjani Bhavesh Variya Snehal Patel Suja Mulamkattil Harsh Amin Shital Butani Ahmed Allam Jamaan Ajarem Harsh Shah 《Molecules (Basel, Switzerland)》2022,27(4)
Non-steroidal anti-inflammatory drugs (NSAIDs) are generally utilized for numerous inflammatory ailments. The long-term utilization of NSAIDs prompts adverse reactions such as gastrointestinal ulceration, renal dysfunction and hepatotoxicity; however, selective COX-2 inhibitors prevent these adverse events. Various scientific approaches have been employed to identify safer COX-2 inhibitors, as in any case, a large portion of particular COX-2 inhibitors have been retracted from the market because of severe cardiovascular events. This study aimed to develop and synthesize a novel series of indomethacin analogues with potential anti-inflammatory properties and fewer side effects, wherein carboxylic acid moiety was substituted using DCC/DMAP coupling. This study incorporates the docking of various indomethacin analogues to detect the binding interactions with COX-2 protein (PDB ID: 3NT1). MD simulation was performed to measure the stability and flexibility of ligand–protein interactions at the atomic level, for which the top-scoring ligand–protein complex was selected. These compounds were evaluated in vitro for COX enzymes inhibition. Likewise, selected compounds were screened in vivo for anti-inflammatory potential using the carrageenan-induced rat paw oedema method and their ulcerogenic potential. The acute toxicity of compounds was also predicted using in silico tools. Most of the compounds exhibited the potent inhibition of both COX enzymes; however, 3e and 3c showed the most potent COX-2 inhibition having IC50 0.34 µM and 1.39 µM, respectively. These compounds also demonstrated potent anti-inflammatory potential without ulcerogenic liability. The biological evaluation revealed that the compound substituted with 4-nitrophenyl was most active. 相似文献
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Rathore Vikas Patel Divyesh Butani Shital Nema Sudhir Kumar 《Plasma Chemistry and Plasma Processing》2021,41(3):871-902
Plasma Chemistry and Plasma Processing - Presently, the world is using different types of disinfectants for various applications such as disinfecting instrument surfaces in the medical field,... 相似文献
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Butani S. C. Vekariya M. K. Dholaria P. V. Kapadiya K. M. Desai N. D. 《Russian Journal of Organic Chemistry》2022,58(6):878-883
Russian Journal of Organic Chemistry - A series of 6-aryl-2-(6-fluoro-3,4-dihydro-2H-1-benzopyran-2-yl)imidazo[2,1-b][1,3,4]thiadiazoles were synthesized through a two-step procedure. The structure... 相似文献
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Butani S. C. Vekariya M. K. Dholaria P. V. Kapadiya K. M. Desai N. D. 《Russian Journal of Organic Chemistry》2022,58(3):405-411
Russian Journal of Organic Chemistry - In an effort to find a new pharmacologically dynamic molecule, we report here the synthesis and in vitro antimicrobial activity of... 相似文献
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