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Biomedical subjects

M Cole

Publications and source records attributed to M Cole.

At least 199 records · Page 11Linked to original sources
PubMed1975

Preparation, hydrolysis, and oral absorption of alpha-carboxy esters of carbenicillin.

Twelve alpha-carboxy esters of carbenicillin, a parenteral broad spectrum semisynthetic penicillin, were synthesized and examined as potential oral carbenicillin derivatives. The rates at which the esters were hydrolyzed in vitro to carbenicillin by animal and human tissues were compared and the carbenicillin serum levels arising after oral administration of the esters were measured in squirrel monkeys and human volunteer subjects. The alpha-carboxyphenyl ester of carbenicillin [carfecillin (British Pharmacopoeia approved name), BRL 3475] WAS SELECTED FOR FURTHER STUDY AND IS PRESENTLY UNDERGOING CLInical trial.

Absorption↗
PubMed1975

Optic ataxia: clinical-radiological correlations with the EMIscan.

After coronary by-pass surgery, a 47 year old, right-handed man developed Gerstmann's syndrome, a visual-spatial perceptual deficit, and a gross impairment of movememt under visual guidance ("optic ataxia"). Visual fields and extraocular movements were intact; he had a left hemiparesis. The EMIscan showed three lesions: a left parietal-occipital lesion; a posterior callosal lesion, and a right frontal lesion. It is hypothesized that optic ataxia in both visual fields requires bilateral lesions which, in the present case, were strategically placed so as to effectively disconnect motor cortex from visual input.

Ataxia↗
PubMed1973

Metabolism of penicillins to penicilloic acids and 6-aminopenicillanic acid in man and its significance in assessing penicillin absorption.

Penicillins can be metabolized to penicilloic acids in man, the extent being dependent on the penicillin structure. In the phenoxy penicillin series, phenoxymethyl penicillin was found to be particularly unstable, but the higher homologues were more stable. In the isoxazolyl series, oxacillin was unstable, and progressive insertion of halogen in the phenyl ring increased stability. Ampicillin and amoxycillin showed some instability, ampicillin possibly being the more stable. After intramuscular administration, carbenicillin was very stable in the body, ampicillin was fairly stable, and benzyl penicillin was unstable. It is important to take into account the penicilloic acid content of urine when estimating total absorption of a penicillin. Increased stability in the body as well as slower renal clearance can lead to high concentrations in the serum. Penicilloic acids seemed to be more slowly cleared from the body than penicillins. The liver is probably the site of inactivation.

Absorption↗
PubMed1973

Prasinons A and B: potent insecticides from Streptomyces prasinus.

Two metabolites which have high activity against sheep blowfly larvae (Lucilia sericata and L. cuprina) were found to be produced by Streptomyces prasinus NCIB 10719. These substances were isolated from culture filtrate by solvent extraction and chromatography and named prasinons A and B. Fermentation factors affecting the formation of these substances are described together with their physical, chemical, and biological properties.

Animals↗
PubMed1972

Inhibition of the -lactamases of Escherichia coli and Klebsiella aerogenes by semi-synthetic penicillins.

1. A new automated micro-iodometric method is described for screening compounds for inhibitory action against beta-lactamase enzymes. 2. Over 1000 semi-synthetic penicillins were tested for inhibitory activity against the beta-lactamase of Escherichia coli B11 and 18 showed a fractional inhibition similar to or higher than that of methicillin. 3. The best inhibitors were alkoxy- and halogen-substituted phenyl-, naphthyl- or quinolyl-penicillins. 2-Isopropoxy-1-naphthylpenicillin (BRL 1437) was clearly the best and had a K(i) value about 1% of that of methicillin. 4. The inhibition of the beta-lactamase of E. coli B11 by BRL 1437 was shown to be reversible and competitive. The K(i) was 0.004mum and K(i)/K(m) with ampicillin and p-hydroxyampicillin (BRL 2333) was about 0.0001. The K(m) and V(max.) values were determined for the beta-lactamases of E. coli B11 and Klebsiella aerogenes A against a variety of penicillins. Cell-bound and solubilized enzymes gave similar K(i) and K(m) values. 5. BRL 1437 was superior to cloxacillin and methicillin for inhibition of the beta-lactamase of live, fully grown cultures of several strains of E. coli and K. aerogenes. Of a group of inhibitors BRL 1437 was the most stable to the beta-lactamase of E. coli B11.

Automation↗
PubMed1972

Microbial metabolites with insecticidal properties.

A screen of fungi for insecticidal activity revealed the ability of Aspergillus versicolor to make versimide, methyl-alpha-(methylsuccinimido)acrylate, a novel contact insecticide. The larvicidal activities of Alternaria tenuis and Fusarium lateritium were found to be due to tenuazonic acid and diacetoxyscirpenol, respectively. Thiolutin, cycloheximide, rubratoxin, patulin, trichothecin, an actinomycin, and scirpene-producing fungi also had insecticidal activity.

Animals↗