99359-37-2Relevant articles and documents
Copper-Catalyzed Cross-Coupling of Secondary α-Haloamides with Terminal Alkynes: Access to Diverse 2,3-Allenamides
Lv, Yunhe,Pu, Weiya,Zhu, Xueli,Zhao, Tiantian,Lin, Feifei
supporting information, p. 1397 - 1401 (2018/02/19)
A copper-catalyzed C(sp)?C(sp3) cross-coupling of terminal alkynes with readily available secondary α-haloamides for the efficient synthesis of 2,3-allenamides is realized. The methodology is characterized by its wide substrate scope, which makes it an important complement to traditional methods for synthesizing allenes. A mechanism involving an alkynylcopper species is proposed. (Figure presented.).
Facile expeditious one-pot synthesis and antifungal evaluation of disubstituted 1,2,3-triazole with two amide linkages
Kaushik,Luxmi, Raj
supporting information, p. 2225 - 2231 (2017/11/15)
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.
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.
