Metabolism of N-Acylated and O-Alkylated Drugs by the Intestinal Microflora During Anaerobic Incubation in vitro

Abstract

1. The ability of the rat intestinal microflora to deacylate or dealkylate a large number of drugs and related compounds during anaerobic incubation in vitro has been explored.

2. Evidence was obtained that the rat microflora is able to deacylate phenacetin and certain related compounds to the corresponding primary amines in vitro. Other N-acylated drugs investigated were found to be resistant to microbial deacylation.

3. Of the O-alkylated compounds studied only certain of those possessing a simple benzenoid structure were susceptible to microfloral degradation. None of the N-alkylated drugs studied were dealkylated by the microflora.

4. The influence of substitution on the susceptibility of drug molecules to microfloral degradation is discussed.