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

GÖKNİL PELİN COŞKUN, HASAN ERDİNÇ SELLİTEPE, BAHİTTİN KAHVECİ, MERT ÜLGEN, İNCİ SELİN DOĞAN

Acta Pharmaceutica Sciencia - 2022;60(4):437-449

Department of Pharmaceutical Chemistry, Faculty of Pharmacy, Acibadem Mehmet Ali Aydınlar University, İçerenköy, Istanbul, Turkey

 

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.