Crooks P A, Godin C S, Damani L A, Ansher S S, Jakoby W B
College of Pharmacy, Division of Medicinal Chemistry and Pharmacognosy, University of Kentucky, Lexington 40536-0082.
Biochem Pharmacol. 1988 May 1;37(9):1673-7. doi: 10.1016/0006-2952(88)90426-1.
Catalytic activities of two amine N-methyltransferases were documented for the following azaheterocycles: isomeric phenyl- and bispyridyls; 2-, 3- and 4-mono-substituted pyridines; and a miscellaneous group of azaheterocycles that included mono- and diazabenzenes and mono- and diazanaphthalenes. The broad substrate specificities of the two amine N-methyltransferases for primary and secondary amines are here extended to a large number of aromatic azaheterocycles in which N-methylation results in the formation of quaternary ammonium metabolites. Pyridine was the best substrate for both enzymes. Substitution in the ring at the 2-position sterically hindered methylation of the pyridyl nitrogen; 2-phenylpyridine and 2,2'-bispyridyl were not substrates.
记录了两种胺N-甲基转移酶对以下氮杂环化合物的催化活性：异构的苯基和联吡啶；2-、3-和4-单取代吡啶；以及一组杂类氮杂环化合物，包括单氮苯和二氮苯以及单氮萘和二氮萘。这两种胺N-甲基转移酶对伯胺和仲胺的广泛底物特异性在此扩展到大量芳香族氮杂环化合物，其中N-甲基化导致形成季铵代谢物。吡啶是这两种酶的最佳底物。在2-位的环取代在空间上阻碍了吡啶氮的甲基化；2-苯基吡啶和2,2'-联吡啶不是底物。
