Drug action phenols

The effect of administration route on drug action is discussed in some detail by Benet (19) and by Rowland (20). Oral administration forces a first-pass route through the liver, subjecting the toxicant to enhanced metabolism. Other routes are weaker metabolically, though in some cases, skin can display up to 80% or more of liver metabolite activity. In the rat, for example, skin is more efficient than liver in degrading aryl carbamates. Our results support this thesis in terms of mean Log MW/LD50 values for phenol toxicity but not for carbamate toxicity. 

Various bioisosteric replacements for a phenolic hydroxyl have been explored. One such, a lactam NH, is incorporated into the design of the 3-adrenergic blocker, carteolol O)- The fundamental synthon is carbostyril derivative K This is reacted in the usual manner with epichlorohydrin to give which is in turn reacted with t-butylamine to complete the synthesis of carteolol (3 ), a drug that appears to have relatively reduced nonspecific myocardial depressant action. Carrying this de-... 

The possession of surface activity per se may be an important faetor in the antibacterial action of a group of drugs, for example the eationie detergents. The addition of low concentrations of surface-active compounds may potentiate the biological effect of an antibacterial agent. Thus, phenols are often more aetive in the presence of soaps. 

Bithionol (Actamer) is a phenolic derivative whose mode of action is related to uncoupling of parasite-specific fumarate reductase-mediated oxidative phosphorylation. The drug is administered orally and is absorbed from the intestinal tract. Peak blood levels are achieved in 4 to 8 hours. Excretion is mainly by the kidneys. 

Eugenol, like other phenolic compounds, is a structurally non-specific drug. The pharmacological action is not directly subordinated to chemical structure, except to the extent that structure affects physicochemical properties, as adsorption, solubility, pKa, and oxidation-reduction potential, factors which influence permeability, depolarization of the membrane and protein coagulation [34],... 

Boehm E, Williams R. A study of the Inhibiting actions of propyl gallate (normal propyl trlhydroxy benzoate) and certain other trlhydrlc phenols on the autoxidation of animal and vegetable oils. Chemist Drug 1943 140 146-147. 

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