Department of Chemistry, Faculty of Science, PO Box 426 Ibrahimia, Alexandria University, Egypt.
Carbohydr Res. 2010 Nov 22;345(17):2474-84. doi: 10.1016/j.carres.2010.08.010. Epub 2010 Oct 9.
The synthesis of a new series of acyclic triazoloquinoxalinyl C-nucleosides and their transformation to their cyclic analogs are described following protection, activation, and deprotection with subsequent intramolecular nucleophilic substitution protocol. The antibacterial potency of the new compounds was determined using an inhibition zone diameter test. The results show that 3a and 2b exhibit good activity against Escherichiacoli and Candidaalbicans. On the other hand, the cyclic mesylated C-nucleoside 13 showed activity against the Gram-positive bacteria (Staphylococcusaureus) and antifungal activity against C. albicans.
描述了一系列新型无环三唑并喹喔啉基 C-核苷的合成及其通过保护、激活和去保护以及随后的分子内亲核取代反应转化为环状类似物的过程。采用抑菌圈直径试验测定了新化合物的抗菌效力。结果表明,3a 和 2b 对大肠杆菌和白色念珠菌表现出良好的活性。另一方面,环状甲磺酸基 C-核苷 13 对革兰氏阳性菌(金黄色葡萄球菌)具有活性,并对白色念珠菌具有抗真菌活性。