38651-27-3Relevant academic research and scientific papers
Facile expeditious one-pot synthesis and antifungal evaluation of disubstituted 1,2,3-triazole with two amide linkages
Kaushik,Luxmi, Raj
, p. 2225 - 2231 (2017)
A library of twenty five amide linked 1,4-disubstituted 1,2,3-triazoles have been prepared through a facile expeditious synthetic protocol involving Cu(I) mediated cyclization of N-(2-methylbut-3-yn-2-yl)aromatic amides and in situ generated 2-azido-N-substituted propanamides. Structures of newly synthesized compounds (5a–5y) were confirmed by analytical techniques, such as FTIR, 1H NMR, 13C NMR, and HRMS. In vitro antifungal activity was also examined against two fungal strains Candida albicans and Aspergillus niger by serial dilution method. The compounds 5 m and 5w exhibited appreciable potent activity.
Synthesis and Antimicrobial Activity of 2-(4-(Hydroxyalkyl)-1H-1,2,3-triazol-1-yl)-N-substituted propanamides
Kaushik,Luxmi, Raj
, p. 3618 - 3625 (2017)
A series of 21 2-(4-(hydroxyalkyl)-1H-1,2,3-triazol-1-yl)-N-substituted propanamides (1,4-disubstituted 1,2,3-triazoles having amide linkage and hydroxyl group) have been synthesized from click reaction between terminal alkyne and 2-azido-N-substituted propanamide (generated in situ from reaction of 2-bromo-N-substituted propanamide and sodium azide) and characterized by FTIR, 1H NMR, 13C NMR spectroscopy, and HRMS. All the newly synthesized triazoles were tested in vitro for antimicrobial activity against four bacterial cultures – Escherichia coli, Enterobacter aerogenes, Klebsiella pneumoniae, and Staphylococcus aureus – and two fungal cultures – Candida albicans and Aspergillus niger. The synthesized 1,4-disubstituted 1,2,3-triazoles displayed moderate to good antimicrobial potential against the tested strains.
Unbalanced-Ion-Pair-Catalyzed Nucleophilic Fluorination Using Potassium Fluoride
Hammond, Gerald B.,Li, Wangbing,Lu, Zhichao,Xu, Bo
supporting information, p. 9640 - 9644 (2021/12/14)
An unbalanced ion pair promoter (e.g., tetrabutylammonium sulfate), consisting of a bulky and charge-delocalized cation and a small and charge-localized anion, greatly accelerates nucleophilic fluorinations using easy handling KF. We also successfully converted an inexpensive and commercially available ion-exchange resin to the polymer-supported ion pair promoter (A26–SO42–), which could be reused after filtration. Moreover, A26–SO42– can be used in continuous flow conditions. In our conditions, water is well-tolerated.
Design and synthesis of new 8-anilide theophylline derivatives as bronchodilators and antibacterial agents
Hayallah, Alaa M.,Talhouni, Ahmad A.,Abdel Alim, Abdel Alim M.
, p. 1355 - 1368 (2013/01/15)
Theophylline derivatives have long been recognized as potent bronchodilators for the relief of acute asthma. Recently, it was found that bacterial infection has a role in asthma pathogenesis. The present work involves the design and synthesis of 8-substituted theophylline derivatives as bronchodilators and antibacterial agents. The chemical structures of these compounds were elucidated by IR, 1H-NMR, mass spectrometry, and elemental analyses. The bronchodilator activity was evaluated using acetylcholine-induced bronchospasm in guinea pigs, and most of the compounds showed significant anti-bronchoconstrictive activity in comparison with standard aminophylline. In addition, the antibacterial activity of all the target compounds was investigated in vitro against Gram-positive and Gram-negative bacteria using ampicillin as a reference drug. Results showed that some of the tested compounds possessed significant antibacterial activity. A pharmacophore model was computed to obtain useful insight into the essential structural features of bronchodilator activity. A structure activity relationship was also discussed.
