The relationship between chemical structure and biological activity of leucomycins and their derivatives was examined
in vivo and
in vitro. The biological activity of Fr-group was higher than that of Ac-group
in vitro, but the latter showed higher blood level and lower toxicity than Fr-group. Lengthening of the carbon chain in the O-acyl group at C-4 in mycarose resulted in a marked increase in the biological activity in vitro, with the isovaleryl group having the highest activity. The aldehyde group in the lactone was related to antibiotic activity, but α, β, γ, δ-unsaturated alcohol system at C
9- to C
12-positions was not important.
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