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Glycopeptide derivatives.
Second-generation glycopeptides, namely LY333328 (Eli Lilly) and BI 397 (Biosearch Italia), which are currently undergoing clinical trials in humans for their promising activity against VanA enterococci, staphylococci (BI 397), and penicillin-resistant pneumococci are focused on. Expand
Ramoplanin (A/16686): a new glycolipodepsipeptide antibiotic from actinoplanes
Etude de la structure de la ramoplanine, un nouvel antibiotique obtenu par fermentation d'Actinoplanes, grâce a des methodes chimiques combinees a de la spectrometrie. Les activites antimicrobiennesExpand
Synthesis and biological evaluation of new fragments from kirromycin antibiotic.
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. Expand
Structure-activity studies of 16-methoxy-16-methyl prostaglandins.
These studies indicate that the introduction of the methyl and methoxy groups at C-16 into the prostaglandin analogues markedly increases the ratio of antisecretory to diarrheogenic action. Expand
Degradation studies of antibiotic MDL 62,879 (GE2270A) and revision of the structure
Abstract Fragments of the thiopeptide antibiotic MDL 62,879 (GE2270A) were prepared under mild degradation conditions. Their structures were determined by spectroscopic techniques and by comparisonExpand
Antibiotics GE23077, novel inhibitors of bacterial RNA polymerase. Part 3: Chemical derivatization.
The current SAR study has identified moieties important for RNA polymerase activity that are based on the lack of penetration of the molecule across the bacterial membrane, owing to its strong hydrophilic character. Expand
Synthesis and preliminary biological characterization of new semisynthetic derivatives of ramoplanin.
Many of the new ramoplanin derivatives showed antimicrobial activity similar to that of the natural precursor coupled with a significantly improved local tolerability, and the derivative in which the 2-methylphenylacetic acid has replaced the di-unsaturated fatty acid side chain was selected as the most interesting compound. Expand
Studies on the luteolytic activity of MDL-646, a new gastroprotective PGE1 analogue, in the hamster.
The biological and biochemical data clearly demonstrate that these 16-methyl-16-methoxy PGE derivatives, given s.c. or p.o. either once or for 3 days, have no luteolytic effects up to a daily dose of 2-2.5 mg/kg, and are therefore at most 1/2 to 1/4 as lutenolytic as the parent natural PGEs. Expand
Ramoplanin (A-16686), a new glycolipodepsipeptide antibiotic. III. Structure elucidation.
The structures of the three components of the antibiotic ramoplanin (A-16686), produced by Actinoplanes sp. Expand
X-ray structure determination of mexiprostil, a new gastroprotective 16-methoxy-16-methyl-PGE1 analogue.
Mexiprostil is a new gastroprotective 16-methoxy-16-methyl-PGE1 methyl ester and X-ray diffraction results established that the configuration at C-15 is also R. Expand