title: Synthesis and biological evaluation of novel 1,2,4-triazine derivatives bearing carbazole moiety as potent α-glucosidase inhibitors.
abstract: A new series of 1,2,4-triazine derivatives bearing carbazole moiety 7a-7p were designed, synthesized, and evaluated for their α-glucosidase inhibitory activity. The majority of the screened compounds displayed potent α-glucosidase inhibitory activity, with IC50 values in the range of 4.27±0.07-47.75±0.25μM as compared to the standard drug acarbose. Among the series, compound 7k represented the most potent α-glucosidase inhibitory activity with IC50 values of 4.27±0.07μM. Kinetic analysis revealed that compound 7k is a non-competitive inhibitor with a Ki of 4.43μM. Furthermore, the binding interactions of compound 7k with α-glucosidase was confirmed through molecular docking. This study showed these 1,2,4-triazine derivatives bearing carbazole moiety as a new class of α-glucosidase inhibitors.
authors.affiliation: College of Chemistry and Chemical Engineering, Jishou University, Jishou 416000, PR China. Electronic address: wanggch123@163.com.
authors.forename: Guangcheng
authors.initials: G
authors.lastname: Wang
authors.affiliation: College of Chemistry and Chemical Engineering, Jishou University, Jishou 416000, PR China.
authors.forename: Jing
authors.initials: J
authors.lastname: Wang
authors.affiliation: College of Chemistry and Chemical Engineering, Jishou University, Jishou 416000, PR China.
authors.forename: Dianxiong
authors.initials: D
authors.lastname: He
authors.affiliation: College of Chemistry and Chemical Engineering, Jishou University, Jishou 416000, PR China.
authors.forename: Xin
authors.initials: X
authors.lastname: Li
authors.affiliation: College of Chemistry and Chemical Engineering, Jishou University, Jishou 416000, PR China.
authors.forename: Juan
authors.initials: J
authors.lastname: Li
authors.affiliation: College of Chemistry and Chemical Engineering, Jishou University, Jishou 416000, PR China.
authors.forename: Zhiyun
authors.initials: Z
authors.lastname: Peng
mesh_terms: D002227:Carbazoles / Q000737:chemistry / Q000494:pharmacology*; D004305:Dose-Response Relationship, Drug; D065089:Glycoside Hydrolase Inhibitors / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology*; D006801:Humans; D062105:Molecular Docking Simulation; D015394:Molecular Structure; D012441:Saccharomyces cerevisiae / Q000201:enzymology; D013329:Structure-Activity Relationship; D014227:Triazines / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology*; D000520:alpha-Glucosidases / Q000378:metabolism*
chemical_list: D002227:Carbazoles; D065089:Glycoside Hydrolase Inhibitors; D014227:Triazines; C041514:carbazole; C093444:1,2,4-triazine; D000520:alpha-Glucosidases
keywords: 1,2,4-Triazine; Carbazole; Enzyme kinetic study; Molecular docking; α-Glucosidase inhibitor