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ACTA Pharmaceutica Sciencia 2022 , Vol 60 , Num 4
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
Göknil Pelin Coşkun 1 Hasan Erdinç Sellitepe 2 Bahittin Kahveci 3 Mert Ülgen 1 İnci Selin Doğan 2
1 Department of Pharmaceutical Chemistry, Faculty of Pharmacy, Acibadem Mehmet Ali Aydınlar University, 34684, İçerenköy, Istanbul, Turkey
2 Department of Pharmaceutical Chemistry, Faculty of Pharmacy, Karadeniz Technical University, 61100, Trabzon, Turkey
3 Department of Nutrition and Dietetics, Karadeniz Technical University, Faculty of Health Sciences 61080, Trabzon, Turkey
DOI : 10.23893/1307-2080.APS6028 Metabolic formation of N-oxides has always been important because of their biological activity profiles. Many N-oxide derivatives today are registered on the market for their diverse clinical use. Tertiary amines and ring nitrogens are main structures 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. Keywords : in vitro metabolism, N-oxide, 1,2,4-triazolo[4,3-a]quinoxaline

Istanbul Medipol University