Department of Chemistry, CQFB-REQUIMTE, Faculty of Sciences and Technology, Universidade Nova de Lisboa, Campus de Caparica, Quinta da Torre, 2829-516 Caparica, Portugal.
Microbiology and Biotechnology Laboratory, Center for Biodiversity, Functional and Integrative Genomics, Faculdade de Ciências, Universidade de Lisboa, Campo Grande, 1749-016 Lisboa, Portugal.
Bioorg Med Chem Lett. 2014 Jan 1;24(1):49-53. doi: 10.1016/j.bmcl.2013.12.002. Epub 2013 Dec 8.
A set of α-quaternary 3-chloro-1-hydroxyalkylphosphonates, analogues of fosfomycin and fosfonochlorin, some of which are new compounds, was synthesized. The compounds were screened for bioactivity against several clinical and standard microbial isolates. Some were found to have moderate activity. The activity was higher with phenyl protection of the phosphoryl ester groups and α-phenyl substitution. Compound 11 was as effective or more potent than fosfomycin or chloramphenicol against several Gram-negative bacteria as well as against some Gram-positive ones.
一组α-四元 3-氯-1-羟烷基膦酸盐，是磷霉素和磷氯苯的类似物，其中一些是新化合物，被合成出来。这些化合物针对几种临床和标准微生物分离株进行了生物活性筛选。一些化合物具有中等活性。当膦酸酯基团被苯保护且α-苯基取代时，活性更高。化合物 11 对几种革兰氏阴性菌以及一些革兰氏阳性菌的活性与磷霉素或氯霉素相当或更强。
