Acceptance rate | 46% |
---|---|
Time to first decision | 6 months* |
Time to decision with review | 50 days* |
*Approximate number of days
**The days mentioned above are averages and do not indicate exact durations. The process may vary for each article.
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
1 Department of Pharmaceutical Chemistry, Faculty of Pharmacy, Acibadem Mehmet Ali Aydınlar University, 34684, İçerenköy, Istanbul, Turkey2 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 Viewed : 8392 - Downloaded : 2389 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