RESUMEN
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.
Asunto(s)
Antibacterianos/biosíntesis , Cicloheptanos/biosíntesis , Nucleotidiltransferasas/antagonistas & inhibidores , Streptomyces/metabolismo , Tropolona/biosíntesis , Antibacterianos/farmacología , Bacterias/efectos de los fármacos , Fenómenos Químicos , Química Física , Sinergismo Farmacológico , Fermentación , Tropolona/análogos & derivados , Tropolona/farmacologíaRESUMEN
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.
