Sung S Y, Kist M, Frahm A W
Albert-Ludwigs-University, Department of Pharmaceutical Chemistry, Freiburg, Germany.
Arch Pharm (Weinheim). 1997 Jan-Feb;330(1-2):21-4. doi: 10.1002/ardp.19973300106.
The stereoisomers of amidinomycin 7 and their intermediates 1-6, which are produced from homochiral 3-oxocyclopentanecarboxylic acids by asymmetric synthesis, are tested for their antimicrobial effects by agar diffusion test and by Bouillon serial dilution assay. Their antibiotic activities against Bacillus subtilis, Staphylococcus aureus, and Micrococcus Iuteus, respectively, are reported. Structure-activity relationships depend on the type and combination of functional groups, on only the relative stereochemistry as well as on the grade of lipophilia of the tested compounds.
由同手性3-氧代环戊烷羧酸通过不对称合成制备的脒霉素7的立体异构体及其中间体1-6，通过琼脂扩散试验和肉汤连续稀释测定法测试其抗菌效果。分别报道了它们对枯草芽孢杆菌、金黄色葡萄球菌和藤黄微球菌的抗菌活性。构效关系取决于官能团的类型和组合、仅取决于相对立体化学以及所测试化合物的亲脂性等级。
