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Biomedical subjects

J Ide

Publications and source records attributed to J Ide.

36 records · Page 2Linked to original sources

Studies on orally active cephalosporin esters.

The synthesis and the biological properties of orally active cephalosporin esters are described. 3-Methoxymethyl cephem derivatives having a 2-(2-aminothiazol-4-yl)-(Z)-2-methoxyiminoacetamide function at C-7 (1) showed good activity against a wide variety of bacteria including some beta-lactamase producing species. The prodrug type esters of 1 exhibited a good urinary recovery after oral administration to mice and 1-(isopropoxycarbonyloxy)ethyl ester (2a, CS-807) has been pre-clinically tested as an orally active cephem prodrug.

Administration, Oral↗

Milbemycins, a new family of macrolide antibiotics. Fermentation, isolation and physico-chemical properties of milbemycins D, E, F, G, and H.

Strain Au-3, a mutant of Streptomyces hygroscopicus subsp. aureolacrimosus, obtained with ultraviolet irradiation, was a high-yield strain of milbemycins D, E, F, G and H. Fermentation studies on the strains were conducted in shake flasks and 30-liter jar fermentors. Isolation of the metabolites was performed by adsorption on resinous adsorbent followed by elution with aqueous MeOH and separated by silica gel column chromatography. Milbemycin D was obtained as colorless needles after recrystallization and milbemycins E, F, G and H were purified to homogeneity by column chromatography. Physico-chemical characterization revealed that milbemycins D, E, F, G and H were new antibiotics possessing the 16-membered macrocyclic lactone with a 6,6-membered spiroketal ring system.

Anti-Bacterial Agents↗

Milbemycins, a new family of macrolide antibiotics. Structure determination of milbemycins D, E, F, G, H, J and K.

The milbemycins, a group of potent, broad-spectrum antiparasitic and pesticidal agents, are architecturally novel antibiotics of 16-membered macrocyclic lactone. Seven new milbemycin analogues designed as milbemycins D, E, F, G, H, J and K were isolated from the fermentation broth of the mutant strain of Streptomyces hygroscopicus subsp. aureolacrimosus. The structural determination of these new components was made mainly by comparing with mass spectra, and 1H and 13C NMR spectra of milbemycin alpha- and beta-series previously published from our laboratory. Milbemycins D, E, F, G and H have characteristically an isopropyl side chain at C-25 which differs from the known milbemycin family bearing methyl or ethyl group at C-25. Milbemycins J and K possess a ketone group at C-5 instead of a hydroxyl or methoxy group. Apart from X-ray crystallography, the R-configuration of the hydroxyl group at C-5 could be best explained both by application of CD allylic benzoate method to the n-N, N-dimethylaminobenzoate of milbemycin D and by comparison of the specific rotation of milbemycin D itself and its acetate with the epimeric isomers at C-5.

Anti-Bacterial Agents↗

Apophysitis of the acromion.

We treated three patients with apophysitis of the acromion. These patients were two male athletes 12 and 14 years of age, respectively, and one female athlete 13 years of age. They reported pain at the top of the shoulder during and after shoulder movement while playing sports but had no rest pain or disturbance of daily activities. Physical examination demonstrated marked local tenderness at the acromion and slight warmth. X-ray films showed sclerosis and irregularity of the secondary ossification center of the acromion. Bone scintigraphy carried out on one patient demonstrated increased uptake in that region. Conservative treatment was used for these patients. Recovery was gradual but satisfactory.

Acromion↗