A Study of the Influence of 96 Compounds From Different Pharmacological Groups on the Acetylation of Aromatic Amines in Vitro
DOI:
https://doi.org/10.5644/Radovi.59Abstract
Taking the action of a compound on the CoA-dependent enzymic acetylation of sulfanilamide as a test tor the ability to interfere with other CoA-dependent processes a screening of a variety of substances from various pharmacological groups has been carried out by the method of Kaplan and Lipmann (14). Especially neuro — and psychophairmaca, as well as a number of poisons acting indirectly on the nervous system, have been tested in view of the fact that the biosynthesis of acetylcholine in nervous tissues is also a CoA-dependent process. A series of aromatic derivatives of acetic and acetohydroxamic acids have been included because such substances have already been reported to inhibit the acetylation of sulphanilamide and choline (8,9,3). AH substances of this type have been found to act as inhibitors (Tab. 3). A great number of the substances tested were devoid of any activity (Tab. 1), but several have shown definite inhibitory action, with one exception, where the action was potentiating (Tab. 2). It is pointed out as striking that there are several pairs of closely related substances, the first of which is inactive, the other an inhibitor, with: adrenaline—noradrenaline, adrenoxyl—adrenochrome, LSD—BOL and SKF-525A—diphenylpropylacetic acid. The only substance found to potentiate the acetylation reaction, 4-hydroxycoumarine, also has a closely related inactive partner, dicoumarol. 4-Hydroxycoumarine has been shown earlier to possess analgetic activity.
References
Altschiil R., Z. Kreislaufforsch., 45, 573 (1956)
Beinert H., v. Korff R. W., Green D. E., Buyske D. A., Handschuhmacher R. E., Higgins H. i Strong J. M., J. Biol. Chem., 200, 385 (1953)
Bošković B. i Fuks Z., u pripremi
Cottet J., Redel J., Krum-Heller C. i Tricaud M. E., Buli acad. nat. med., 137, 441 (1953)
Decker K., Die aktivierte Essogsaure, F. Enke Ver., Stuttgart, 1959, str. 36,
Decker K., Die aktivierte Essogsaure, F. Enke Ver., Stuttgart, 1959, str. 267.
Dick E. C., Greenberg S. M., Herndon J. F., Jonas M. i Van Loon E. J., Proc. Soc. exp. biol. med., 104, 323 (1960)
Feldberg W. i Mann T., J. Physiol. (London), 104, 411 (1946)
Garratini S., Morpurgo C., Murelli B., Paoletti R. i Passerini N., Arch. int. pharmacodvn., 109, 400 (1957)
Garratini S. Morpurgo C. i Passerini N., Experientia, 14, 89 (1958)
Gioia A. i Morpurgo C., Brit. J. Pharmacol., 13, 467 (1958)
Grave D., citirano u ref. (15) str. 154.
Helmrech E., Holzer H., Goldschmidt S.; Lamprecht W., i Ritze F., Z. Physoil. Chem., 292, 184 (1953)
Holzer H., Ang. Chem. 64, 248 (1952)
Kaplan N. O. i Lipmann F., J. Biol. Chem., 174, 37 (1948)
Lin T. M. i Chen K. K., Fortschr. Arzneimittelforsch. Vol. I, Birkhauser Veri., Basel, 1959, a) str. 133, b) str. 139.
Lipmann F., J. Biol. Chem., 160, 173 (1945)
Lipmann F. i Kaplan N. O., ibid. 162, 743 (1946)
Lipmann F., Kaplan N. O., Novelli G. D., Tuttle L. C. i Guirard B. M., ibid. 186, 235 (1956)
Lipton M. A. i Barron S. G., ibid. 166, 367 (1948)
Lynen F., Liebigs Ann. 552, 270 (1942)
Lynen F., Federation Proc. 12, 683 (1953)
Lynen F., Reichert E. i Rueff L., Liebigs Ann. 578, 1 (1951)
Markees S. i Meyer F. W., Schweiz. Med. Wschr. 1949, 931
Nachmansohn D. i Berman R., J. Biol. Chem. 165, 551 (1946)
Novelli G. D., Physiol. Rev. 23, 525 (1953)
Novelli G. D. i Hoagland M. B., 123 rd Meeting, Am. Chem. Soc., Los. Angeles, March 1953, Abstr., str. 260
Riggs T. R. i Hegstedt D1. M., J. Biol. Chem. 172, 539 (1948)
Siperstein M. D., Aim. J. Clin. Natr. 8, 645 (1960)
Snell E. E, Brown G. M., Peters V. J., Graig J, A., Wittle El. L., Moore J. A., Mcglohon M. V. i Bird C. D. J., J. Am. Chem. Soc. 76, 3575 (1954)
Stadman E. R. i Kornberg A., J. Biol. Chem. 203, 47 (1953)
Stern P., Ratković D. i Fuks Z., Arch. int. pharmacodyn. 130, 1 (1961)
Stern P., Deželić M., Košak R., Arch. exp. Path. u. PharmakoL 232, 356 (1957)
Tavormina P. A. i Gibbs M., J. Am. Chem. Soc. 79, 758 (1957)
Wagner-Jauregg Th. i Sauer H., Arzneimittelforsch. 9, 575 (1959)
Wieland O., Klin. Wschr. 32, 385 (1954)
Winegard A., Schaw W. N., Lukens F. D. W. i Stadie W. C., Am. Clin. Nutr. 8, 651 (1960)
Downloads
Published
Issue
Section
License
Copyright (c) 2026 Bogdan Bošković, Željko Fuks, Pavao Štern
This work is licensed under a Creative Commons Attribution 4.0 International License.
