Biomedical subjects

R M Bradshaw

Publications and source records attributed to R M Bradshaw.

8 recordsLinked to original sources

PubMed1984

Beta 1-selective adrenoceptor antagonists. 3. 4-Azolyl-linked phenoxypropanolamines.

A series of 4-substituted phenoxypropanolamines has been prepared and examined for beta-adrenoceptor activity. The 4-substituents, di- and triazole ring systems connected to the phenoxy ring by different length chains, were chosen as a means of introducing cardioselectivity. This has been achieved, especially in the 1-[4-[(4-chloropyrazol-1-yl)methoxy] phenoxy]-3-(isopropylamino)-2-propanol (11), the 4-[(2H-1,2,3-triazol-2-yl)methoxy] analogue (21), and the 4-[2-(2H-1,2,3-triazol-2-yl)ethoxy] analogue (22), which show potent beta 1-blockade with selectivity ratios in excess of 100:1. Structure-activity relationships are discussed, and the optimum position of the heteroatom in the 4-substituent is defined.

Adrenergic beta-Antagonists↗

PubMed1983

beta 1-selective adrenoceptor antagonists. 2. 4-ether-linked phenoxypropanolamines.

A series of 4-substituted phenoxypropanolamines was prepared and examined for beta-adrenoceptor activity. Some of the compounds, especially the [4-[2-[[2-(4-fluorophenyl)ethyl] oxy]ethoxy]phenoxy]propanolamines (14, 15, and 24), showed potent beta 1-blockade with virtually no beta 2-blockade at doses over a 1000 times greater. The compounds also possessed partial agonist activity. Structure-activity relationships are discussed, and conclusions are drawn about the binding sites on beta-adrenoceptors.

Adrenergic beta-Agonists↗

PubMed1976

Chemical composition of the spore sheath of Streptomyces griseus.

The fibrillar sheath surrounding spores of Streptomyces griseus was separated from spores and partially purified by differential centrifugation. The reaction of isolated sheath material to various solvents and enzymes was monitored by electron microscopy. Fibrilar elements (rodlets) were apparently resistant to most solvents and enzymes used; only acetone induced any change in their appearance. Analysis of sheath material showed that its composition differed considerably from that of spore walls, having a low content of nitrogen (1.7% w/w), amino sugars (0.067% w/w) and carbohydrate (0.036% w/w). It was suggested that the sheath may be at least partially inorganic in nature.

Amino Sugars↗

PubMed1974