As new compound are now provided ten compounds, namely 1-N-(2R,3R)-4-amino-3-fluoro-2-hydrox ybutyrylkanamycin A; 1-N-((2R,3R)-4-amino-3fluoro-2-hydroxybutyryl-2',3'-dideoxykanamycin A; 1-N-(2R,3R)-4-amino-3-fluoro-2-hydroxybutyryl 2',3'-dideoxy-2'-fluorokanamycin A; 1-N-(2R,3R)-4amino-3-fluoro-2-hydroxybutyryl-5-deoxy-5fluorokanamycin A; 1-N-(2R,3R)-4-amino-3-fluoro-2hydroxybutyryl-kanamycin B; 1-N-((2R,3R)-4-amino 3-fluoro-2-hydroxybutyryl-3'-deoxykanamycin B; 1 N-(2R,3R)-4-amino-3-fluoro-2-hydroxybutyryl-3',4'dideoxykanamycin B; 1-N-((2R,3R)-4-amino-3-fluoro 2-hydroxybutyryl-5-deoxy-5-fluorokanamycin B; 1-N{(2R,3R)-4-amino-3-fluoro-2-hydroxybutyryl-5,3'dideoxy-5-fluorokanamycin B; and 1-NC2R,3R)-4amino-3-fluoro-2-hydroxybutyryl-5,3',4'-trideoxy-5fluorokanamycin B, which are all useful as antibacterial agent in the therapeutic treatment of bacterial infec t1O.S.

57 ABSTRACT 3',4'-a-Epoxyneamine and its related aminoglycosidic antibiotic derivatives containing 3',4'-a-epoxyneamine moiety in the molecule thereof are now provided, which may be in the form of their amino-protected and partially hydroxyl-protected product and which are useful as intermediates for use in the synthetic produc tion of therapeutically valuable 3'-deoxy derivatives of aminoglycosidic antibiotics.

Since the chemical screening of microbial metabolites was first described in the isolation of dienomycinsl' which had antibacterial and local anesthetic activities, a number of new metabolites such as antipain2), arglecin3), and phosphoramidon4) have been found by the screening in our laboratories. In the present paper, we wish to report the isolation and structural elucidation of metabolite KD16-U1 (1). This new metabolite is produced by Streptomyces ftlipinensis5) (the Laboratory No. KD16-C2), and is positive to triphenyltetrazolium chloride (TTC). The screening method used was substantially similar to that described in a previous paper1).

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An inhibitor of phosphatidylinositol-specific phospholipase C (PI-PLC), pholipeptin (1), was purified from the culture broth of Pseudomonas sp. by solvent extraction and column chromatography. Acid hydrolysis of 1 gave Leu, Ile, Ser, Thr, and Asp moieties. Although 1 was a peptide compound, fragmentation by mild hydrolysis was not accomplished under any conditions. So, we performed the structure elucidation using various 2D NMR techniques. In the NMR studies, the addition of a small amount of trifluoroacetic acid gave relatively sharp and resolved signals, such that the structure of this novel cyclic lipodepsipeptide consisting of 11 amino acids and a 3-hydroxydecanoic acid moiety could be determined. Chirality of the constituent amino acids was analyzed by chiral HPLC, but two Asp residues could not be distinguished because they were contained as a racemic mixture. Finally, their chiralities were determined by NMR analysis of (13)C-labeled 1 into which [L-(13)C]Asp had been biosynthetically incorporated.

AbstractChemInform is a weekly Abstracting Service, delivering concise information at a glance that was extracted from about 100 leading journals. To access a ChemInform Abstract of an article which was published elsewhere, please select a “Full Text” option. The original article is trackable via the “References” option.