ASYMMETRIC-SYNTHESIS AND STRUCTURE-ACTIVITY RELATIONSHIP OF THE 4 STEREOISOMERS OF THE ANTIBIOTIC AMIDINOMYCIN .2. MICROBIOLOGICAL TESTING

The stereoisomers of amidinoinycin 7 and their intermediates 1-6, whic h are produced from homochiral 3-oxocyclopentanecarboxylic acids by as ymmetric synthesis, are tested for their antimicrobial effects by agar diffusion test and by Bouillon serial dilution assay. Their antibioti c activities against Bacillus subtilis, Staphylococcus aureus, and Mic rococcus luteus, respectively, are reported. Structure-activity relati onships depend on the type and combination of functional groups, on on ly the relative stereochemistry as well as on the grade of lipophilia of the tested compounds.