Biological Conversion of n-Butyl Penicillin into a Chemotherapeutically Active Substance

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Abstract
Although n-butyl penicillin is almost devoid of in vitro activity against the hemolytic streptococcus, the ester confers marked protection to the mouse infected with lethal dosages of virulent hemolytic streptococci. Following the subcut. injection of 200 mg. of n-butyl penicillin into [male] patients with acute gonorrheal urethritis, no favorable influence on the course of the infections was noted. Appreciable quantities of penicillin could not be detected in either the blood or urine of the dog, monkey, or man after subcut. administration of the ester. It is postulated that the ester itself possesses no ehemotherapeutic activity but that the tissues of the mouse possess the ability to convert this ester by hydrolysis into the chemotherapeutically active free penicillin which then displays its usual activity against streptococcal infections. On the other hand, the tissues of the higher mammals investigated appear not to possess such a hydrolytic system, since the n-butyl penicillin ester does not display any ehemotherapeutic effect in these latter animals. The above results are in agreement with those obtained by Richardson et al. (Jour. Pharmacol. 85: 23, 1945) in the case of the methyl ester. Such results do not appear to hold forth hope for the successful use of penicillin esters in human infections.

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