5-Butylpicolinic acid

Butylpicolinic acid (fusaric acid, 4.68) is a major metabolite of 5-bu-tylpicolinamide (SCH 10985, 4.67) in the plasma of rats, dogs, and humans. The biological activity of this compound (an inhibitor of dopamine-/3-hy-droxylase) is mainly due to its metabolite fusaric acid, indicating that, in this example, the hydrolysis of the amide group is bioactivating [41]. 

The pH dependence of the rates of complex formation between Ni + and picolinic acid (pyridine-2-carboxylic acid) and fusaric acid (5-butylpicolinic acid) are not linear functions of but can be accounted for by a reaction scheme in which initial complexing occurs at the carboxylate group and chelate ring closure is an important kinetic factor (Scheme 2). If the rate law is expiessed in the form — d[Ni2+]/d/ = A obs[Ni][total ligand... 

Methylapogalanthamine (xx), hypotensive in cats, dogs and rabbits, has adrenolytic, spasmolytic and sedative properties. It has been approved for wide clinical use in the U.S.S.rI A naphthoquinone (XXl) from the fungus Corynespora cassicola inhibits catechol-o-methyltransferase in vitro and is a hypotensive of long duration (24 hrs.) in spontaneous hypertensive rats after 12.5 mg/kg l.p. Fusaric acid (5-n-butylpicolinic acid) analogs with chlorine or bromine in the 3- and/or 4-position of the side... 

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