Quantitative structure-activity relationships in erythromycin group with MTD technique

Quantitative structure-activity correlation studies were performed for a group of 17 erythromycin derivatives modified in the C-8--C-12 portion of the molecule. The minimal steric difference, MTD, was used as the structural parameter and logarithm of the biological potency measured by a standard assay, as the biological parameter. The influence of the sp2 hybridization at C-9 and of the presence of 11, 12-carbonate grouping on the antibacterial activity was shown. The reported results give a further support to our hypothesis on greater complementarity of the cyclic 11, 12-carbonates in the reaction on the bacterial ribosomes in comparison with their parent antibiotics.