Laboratory of Applied Organic Chemistry, Synthesis of Biomolecules and Molecular Modelling Group, Badji-Mokhtar-Annaba University, Box 12, 23000 Annaba, Algeria.
Laboratory of Applied Biochemistry and Microbiology, Department of Biochemistry, Badji-Mokhtar-Annaba University, Box 12, 23000 Annaba, Algeria.
Molecules. 2018 Jul 10;23(7):1682. doi: 10.3390/molecules23071682.
Several new sulfamidocarbonyloxyphosphonates were prepared in two steps, namely carbamoylation and sulfamoylation, by using chlorosulfonyl isocyanate (CSI), α-hydroxyphosphonates, and various amino derivatives and related (primary or secondary amines, β-amino esters, and oxazolidin-2-ones). All structures were confirmed by ¹H, C, and P NMR spectroscopy, IR spectroscopy, and mass spectroscopy, as well as elemental analysis. Eight compounds were evaluated for their antibacterial activity against four reference bacteria including Gram-positive (ATCC 25923), and Gram-negative (ATCC 25922), (ATCC 700603), (ATCC 27853), in addition to three clinical strains of each studied bacterial species. Compounds ⁻ and showed significant antibacterial activity compared to sulfamethoxazole/trimethoprim, the reference drug used in this study.
几种新的磺酰胺羰基氧膦酸酯通过两步法，即氨基甲酰化和磺酰胺化，用氯磺酰异氰酸酯（CSI）、α-羟膦酸酯和各种氨基衍生物及其相关物（伯或仲胺、β-氨基酯和恶唑烷-2-酮）制备。所有结构均通过 ¹H、C 和 P NMR 光谱、IR 光谱和质谱以及元素分析得到证实。评估了 8 种化合物对包括革兰氏阳性菌（ATCC 25923）和革兰氏阴性菌（ATCC 25922）、（ATCC 700603）、（ATCC 27853）在内的 4 种参考菌和每种研究菌的 3 种临床株的抗菌活性。与本研究中使用的参考药物磺胺甲恶唑/甲氧苄啶相比，化合物 ⁻ 和 表现出显著的抗菌活性。
