RESUMO
A novel low-molecular weight inhibitor of an aminoglycoside-inactivating enzyme, initially isolated from fermentation broths of Streptomyces neyagawaensis, was determined to be 7-hydroxytropolone. Its structure was confirmed by synthesis. In vitro synergy was demonstrated between 7-hydroxytropolone and certain aminoglycosides against bacteria which were resistant to those aminoglycosides by virtue of a 2"-O-adenylyltransferase. The synthesis and characterization of some analogs of 7-hydroxytropolone is also described.
Assuntos
Antibacterianos/biossíntese , Cicloeptanos/biossíntese , Nucleotidiltransferases/antagonistas & inibidores , Streptomyces/metabolismo , Tropolona/biossíntese , Antibacterianos/farmacologia , Bactérias/efeitos dos fármacos , Fenômenos Químicos , Físico-Química , Sinergismo Farmacológico , Fermentação , Tropolona/análogos & derivados , Tropolona/farmacologiaRESUMO
An inhibitor of dopamine-beta-hydroxylase, designated A32390A, was isolated from the culture broth of a Pyrenochaeta species. The inhibitor showed antimicrobial activity against fungi and gram-positive bacteria. Spectroscopic analysis and chemical degradation studies indicated that the structure was 1,6-di-O-(2-isocyano-3-methylcrotonyl)-D-mannitol.