Izvorni znanstveni članak

Erythromycin Series. X. Inhibitory Activity of Several New Erythromycin Derivatives in Cell-Free Amino Acid Polymerization Systems

P. Matijašević ; PLIVA, Pharmaceutical and Chemical Works, L. Ribara 89, 41000 Zagreb
N. Franjić ; PLIVA, Pharmaceutical and Chemical Works, L. Ribara 89, 41000 Zagreb
S. Đokić ; PLIVA, Pharmaceutical and Chemical Works, L. Ribara 89, 41000 Zagreb
Ž. Kućan ; PLIVA, Pharmaceutical and Chemical Works, L. Ribara 89, 41000 Zagreb

Sažetak

Erythromycin A (I), erythromycin A 9-oxime (11), 9(S)-erythromycylamine
(V), and several new derivatives of these compounds,
were assayed for their ability to inhibit the poly(A)-directed synthesis
of polylysine and the poly(C)-directed synthesis of polyproline
in cell-free systems from Escherichia coli. The rate of polypeptide
synthesis was inhibited 500/o by concentrations between
0.5 and 1.5 ~tmol · dm-3 of the eight examined compounds, in the
following decreasing order of activity: methylsuccinate of V (VI),
I, V, II, methylsuccinate of II (111), p-toluenesulfonyl-V (VII), p-
acetylamino-benzenesulfonyl-V (VIII), and ethylsuccinate of I
(IV). The derivative of VII lacking cladinose (IX) showed lower
but still significant activity. Hence, none of the substitutions in
the position 9 of the macrolide ring, present in these compounds,
impairs the ability of I to bind the prokaryotic ribosome and inhibit
its function, which is the basis for antibacterial activity of erythromycines.

Ključne riječi

Hrčak ID:

194564

URI

https://hrcak.srce.hr/194564

Datum izdavanja:

15.11.1980.

Posjeta: 506 *