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Biomedical subjects

D M BROWN

Publications and source records attributed to D M BROWN.

14 recordsLinked to original sources
PubMed1961

Pharmacology of methicillin.

The pharmacology of a new antibiotic methicillin, 6(2:6-dimethoxybenzamido)-penicillanic acid, which is effective against staphylococci resistant to penicillin G, has been investigated. It is free from acute and chronic toxic effects, except that some pain may be caused following intramuscular injection. It is poorly absorbed orally, but after intramuscular injection the concentrations in the serum and in tissues are very similar to those found with penicillin G. It is excreted by the kidneys both by renal tubular secretion and glomerular filtration. It is also excreted in the bile in very high concentrations, the ratio of concentration in the bile to the blood being approximately 2.5 times that of penicillin G. From a study of the metabolism of the drug it is calculated that 75% is eliminated unchanged in the urine and that the remainder is probably destroyed after the excretion into the intestine via the bile.

Bile↗
PubMed1960

The antitubercular properties of a series of thiols and sulphides.

The antitubercular activity of a series of thiols, dithiolans, thiol esters, dimercaptopropyl esters, and episulphides has been examined in vitro and in vivo in mice infected with the H(37)Rv strain of Mycobacterium tuberculosis. Most of the thiol compounds were inactive, although dimercaprol (2,3-dimercaptopropanol; B.A.L.) and a few closely related compounds showed slight activity in vivo, the only exception being 2,3-dimercaptopropyl chloride which was very active. The dithiolans were inactive, but some of the thiol esters were moderately active, in particular 2,3-di(acetylthio)propyl acetate and 1,2,3-tri(acetylthio)propane. The majority of the dimercaptopropyl esters had significant activity, the most active compounds being 2,3 - dimercaptopropyl benzoate, 1, 3 - dimercapto - 2 - propyl benzoate, 2, 3 - dimercaptopropyl o-chlorobenzoate, and 2,3-dimercaptopropyl p-chlorobenzoate. All the S-acyl derivatives of 3-mercaptopropylene sulphide had good antitubercular activity, some being more active than streptomycin. The most active compound of the series was 3-(2-furoylthio)propylene sulphide. The activity of the compounds is believed to be due to their conversion in vivo to 3-mercaptopropylene sulphide and not due to the formation of ethanethiol. Slight deviation from the basic structure abolishes antitubercular activity.

Acetates↗
PubMed1960

The antitubercular activity of 3-acetylthiopropylene sulphide and 3-(2-furoylthio) propylene sulphide.

Two derivatives of 3-mercaptopropylene sulphide (B.R.L. 482), 3-acetylthiopropylene sulphide (B.R.L. 459) and 3-(2-furoylthio)propylene sulphide (B.R.L. 658), have been tested in mice for antitubercular activity. The compounds were administered daily in arachis oil by the subcutaneous route. When tested by a prolongation in survival time B.R.L. 459 was less active than streptomycin, while B.R.L. 658 was of the same order of activity. When assessed by the lesions present in the lungs after 14 days' treatment B.R.L. 658 was as active as isoniazid and B.R.L. 459 was of the same order of activity as streptomycin. Neither compound, however, cured an established infection and resistance developed rapidly to both compounds, both in vitro and in vivo. It is concluded that, in view of their adverse physical and pharmacological properties, the compounds are unsuitable for clinical use.

Animals↗
PubMed1957

Phramacological properties of esters of 1-alkyl-2-hydroxyalkylpyrrolidine and their quaternary derivatives.

A series of esters of 1-alkyl-2-hydroxyalkylpyrrolidine and their quaternary derivatives have been shown to possess significant anti-acetylcholine activity. The benzilic acid esters were the most active, followed by xanthene-9-carboxylic acid, fluorene-9-carboxylic acid and diphenylacetic acid esters in that order. The quaternary derivatives were more active than their corresponding tertiary compounds both in vivo and in vitro. The most active compound of the series tested in vivo was (1-methylpyrrolid-2-yl)methyl benzilate methiodide and was as potent as atropine. There was a progressive decrease in anti-acetylcholine activity and a proportional increase in local anaesthetic activity as the number of carbon atoms was increased from 1 to 3 in the pyrrolidyl side-chain of the tertiary salts of the benzilic acid ester series. Likewise increasing the size of the group on the nitrogen atom led to a decrease in anti-acetylcholine activity and an increase in local anaesthetic activity. Quaternization of the tertiary salts resulted in a loss of local anaesthetic activity. Most of the compounds tested possessed some antihistamine properties, while papaverine-like activity was confined to the tertiary salts only. No significant neuromuscular blocking activity was evident.

Acetylcholine↗
PubMed1955

Nucleic acids.

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Nucleic Acids↗