Abstract
IN the course of investigations involving sulphonamide acetylation it was observed that the acetylation of sulphanilamide by pigeon liver extracts was markedly inhibited by isoniazid (isonicotinylhydrazide) (unpublished results). By means of the procedure of Lineweaver and Burk1 the inhibition was found to be competitive in nature. The probability that the inhibition was of the competing substrate type was increased by the recent findings of Hughes2 and others3 that, following the administration of isoniazid to man and monkeys, 1-isonicotinyl-2-acetylhydrazine appears in the urine. It has now been found that isoniazid is readily acetylated by pigeon liver extract, and that substances which inhibit sulphanilamide acetylation also inhibit the acetylation of isoniazid.
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References
Lineweaver, H., and Burk, D., J. Amer. Chem. Soc., 56, 658 (1934).
Hughes, Hettie, B., J. Pharmacol. and Exp. Therap., 109, 444 (1953).
Makino, K., Kinoshita, T., and Itoh, T., Nature, 173, 36 (1954).
Johnson, W. J., and Quastel, J. H., Nature, 171, 602 (1953).
Bratton, A. C., and Marshall, E. K., J. Biol. Chem., 128, 537 (1939).
Scott, P. G. W., J. Pharm. and Pharmacol., 4, 681 (1952).
Srere, P. A., and Lipmann, F., J. Amer. Chem. Soc., 75, 4874 (1953).
Thoren, M., and Hinshaw, H. C., Stanford Med. Bull., 10, 316 (1952).
Bernstein, J., Lott, W. A., Steinberg, B. A., and Yale, H. L., Amer. Rev. Tuberc., 65, 357 (1952).
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JOHNSON, W. Biological Acetylation of Isoniazid. Nature 174, 744–745 (1954). https://doi.org/10.1038/174744a0
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DOI: https://doi.org/10.1038/174744a0
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