New N-acyl derivatives of 1-N-desmethyl goldinamine were obtained from degradation of kirromycin. Periodate-oxidation of these derivatives provided new aldehydic fragments that were further elaborated. Both N-phenyl ureido and N-phthalimido derivatives of 1-N-desmethyl goldinamine are able to inhibit bacterial protein synthesis in cell-free assay and are active against whole microorganisms, although with lower potency than kirromycin. The derivatives from the aldehydic fragments are totally inactive.
Synthesis and biological evaluation of new fragments from kirromycin antibiotic / P. Tavecchia, A. Marazzi, C. Dallanoce, A. Trani, I. Ciciliato, P. Ferrari, E. Selva, R. Ciabatti. - In: JOURNAL OF ANTIBIOTICS. - ISSN 0021-8820. - 49:12(1996), pp. 1249-1257. [10.7164/antibiotics.49.1249]
Synthesis and biological evaluation of new fragments from kirromycin antibiotic
C. Dallanoce;
1996
Abstract
New N-acyl derivatives of 1-N-desmethyl goldinamine were obtained from degradation of kirromycin. Periodate-oxidation of these derivatives provided new aldehydic fragments that were further elaborated. Both N-phenyl ureido and N-phthalimido derivatives of 1-N-desmethyl goldinamine are able to inhibit bacterial protein synthesis in cell-free assay and are active against whole microorganisms, although with lower potency than kirromycin. The derivatives from the aldehydic fragments are totally inactive.Pubblicazioni consigliate
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