Catecholamines structure-activity relationship

Structure and activity at adrenergic receptors of catecholamines and related compounds, 2, 127 Structure-activity relationships and mechanism of action of antibacterial sulphanilamides and... 

In view of the known actions of catecholamines on the myocardium and from the observation that the Individual with angina pectoris has a hyperactive sympathetic system, it is rationalized that blockade of the beta adrenergic receptors may benefit the anginal patient. There are a number of agents which produce a selective blockade of the beta adrenergic receptor, their structure activity relationships have been reviewed. 

Melchiorre, C., Belleau, B., 1981. Recent developments in structure-activity relationships among inhibitors of the adrenergic a-receptor. In Kunos, G. (Ed.), Adrenoceptors and Catecholamine Action, Part A. Wiley, New York, pp. 131-179. 

The early pioneering work by Zeller et al. (115) on the potent MAO inhibitory effect of iproniazid—a structural modification of the tuberculostat Isoniazid—and his realization of the physiologic consequences that might arise from such a profound alteration in catecholamine metabolism, the actual confirmation by Brodie, Pletscher, and Shore (27) of the rise in brain monoamine levels following the administration of iproniazid and JB-516 (a-methylphen-ethylhydrazine), and the early euphoric effects noted by Selikoff, Robitzek, and Omstein (96) in tuberculosis patients on iproniazid therapy led Kline and his associates (67) to investigate the possible application of iproniazid in the treatment of mental depression. It was their conclusion that MAO inhibition and antidepressant effect had a causal relationship and that a new approach for the treatment of mental depression had been uncovered. The subject of the MAO inhibitors has been reviewed extensively up to 1960 by Pletscher, Gey, and Zeller (84) and by Biel, Horita, and Drukker (21) to 1963, in comprehensive reviews of the chemistry, biochemistry, pharmacology, clinical application, and structure-activity relationships of the MAO inhibitors. 

Norepinephrine and epinephrine are members of a class of pharmacologically active substances known as catecholamines, because they contain within their structures both an amine and ortho-dihydroxybenzene, which is known by the common chemical name of catechol. Many adrenergic drugs also are catecholamines, and their structure-activity-relationships (SARs) will be discussed. 

J.M. Sanchis Mallols, R.M. Villanueva Camanas, S. Sagrado and M.J. Medina Hernandez, Quantitative Retention-Structure and Retention-Activity Relationship Studies of Ionic and Nonionic Catecholamines by MLC, Chromatographia, 46 605 (1997). 

Flavonoids are widely distributed in fruits and vegetables and are very common nutritional supplements as antioxidants. The results on antioxidant activities of simple catechols provide a useful basis for evaluating results for the many, more complex natural compounds containing the catechol structure, such as the flavonoids, steroidal catechols and hormonal catecholamines. There are several reviews on the antioxidant properties of flavonoids and several reports on experimental " and theoretical evidence linking their antioxidant properties to the catechol moiety usually found in their structure. The basic flavonoid structure (29) is shown in Chart 1, with a few selected examples (30-36) from different groups to illustrate some of the relationships between their detailed structures and related antioxidant properties. Efforts to elucidate these relationships are hampered by their very low solubility in non-polar solvents, and the tendency of some researchers to employ metal ions as initiators of oxidation in aqueous media so that one cannot distinguish between their action as chain-breaking... 

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