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Modification of eremomycin by amine groups

Olsuf'eva, E.N.; Berdnikova, T.F.; Dokshina, N.I.; Lomakina, N.N.; Orlova, G.I.

Antibiotiki i Khimioterapiia 34(5): 352-358

1989

ISSN/ISBN: 0235-2990
PMID: 2742420
Document Number: 340252
Possible modification of eremomycin, a novel glycopeptide antibiotic by the amine groups with acylating agents such as Ac2O/MeOH and CH3(CH2)7COCl/Et3N and alkylating agents such as CH3CHO, NaBH and NaBH3CN was studied. N-Acetyl, N,N'-diacetyl. N-pelargoil, N-ethyl, N,N'-diethyl and N,N',N"-triethyl derivatives of eremomycin were prepared. Their structure was asserted and the order of the substitute introduction was determined. The antimicrobial activity against Bacillus subtilis and Staphylococcus aureus was assayed. It was found that with introduction of the ethyl substitutes to the eremomycin molecule the antibiotic activity lowered insignificantly whereas the acylation resulted in its decreasing by 1-2 orders.

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