Formation of an N-oxide metabolite following metabolism of 1-(3-chlorobenzyl)[1,2,4] triazolo[4,3-a]quinoxaline by in vitro rat liver microsomal preparations

COŞKUN G. P., SELLİTEPE H. E., KAHVECİ B., ÜLGEN M., DOĞAN İ. S.

Acta Pharmaceutica Sciencia, vol.60, no.4, pp.437-449, 2022 (Scopus) identifier

  • Publication Type: Article / Article
  • Volume: 60 Issue: 4
  • Publication Date: 2022
  • Doi Number: 10.23893/1307-2080.aps6028
  • Journal Name: Acta Pharmaceutica Sciencia
  • Journal Indexes: Scopus, EMBASE
  • Page Numbers: pp.437-449
  • Keywords: 1, 2, 3-a]quinoxaline, 4-triazolo[4, in vitro metabolism, N-oxide
  • Karadeniz Technical University Affiliated: Yes

Abstract

© 2022, Istanbul Medipol University. All rights reserved.Metabolic formation of N-oxides has always been important because of their biological activity profiles. Many N-oxide derivatives today are registered on the mar-ket for their diverse clinical use. Tertiary amines and ring nitrogens are main struc-tures in drugs and xenobiotics for metabolic production of N-oxides in biological systems. Recently a new class of quinoxaline derivatives were synthesized and their anti-inflammatory activity was studied. In the present study, we studied in vitro microsomal metabolism of 1-(3-chlorobenzyl)[1,2,4]triazolo[4,3-a]quinoxaline (substrate) selected as the most active compound out of these quinoxaline derivatives using rat liver microsomes. The preliminary results from LC-MS experiments revealed that this substrate underwent N-oxidation in the presence of microsomes and co-factors.