Faculty of Science, Department of Chemistry, Tanta University, Tanta, Egypt.
Arch Pharm (Weinheim). 2012 Oct;345(10):784-9. doi: 10.1002/ardp.201200109. Epub 2012 Jul 24.
Two series of novel α-aminophosphonates having heterocyclic moieties were synthesized in high yields. The structures of the newly synthesized compounds were confirmed by their elemental analyses, IR, (1)H NMR and MS spectral data. These compounds were screened for their antibacterial activities against Escherichia coli (NCIM2065) as a Gram-negative bacterium, Bacillus subtilis (PC1219) and Staphylococcus aureus (ATCC25292) as Gram-positive bacteria, and Candida albicans and Saccharomyces cerevisiae as fungi. The minimum inhibitory concentrations (MICs) of the synthesized compounds show high antibacterial and antifungal activities at low concentrations (10-1000 µg/mL). Furthermore, their lethal doses indicated that such compounds are safe for use as antimicrobial agents.
合成了两个系列具有杂环结构的新型α-氨基膦酸酯，产率高。新合成化合物的结构通过元素分析、IR、（1）H NMR 和 MS 光谱数据得到证实。这些化合物被筛选出对革兰氏阴性菌大肠杆菌（NCIM2065）、革兰氏阳性菌枯草芽孢杆菌（PC1219）和金黄色葡萄球菌（ATCC25292）以及真菌白色念珠菌和酿酒酵母具有抗菌活性。合成化合物的最低抑菌浓度（MIC）在低浓度（10-1000μg/mL）下表现出高抗菌和抗真菌活性。此外，它们的致死剂量表明，这些化合物作为抗菌剂使用是安全的。
