title: Pyridothiadiazine derivatives as aldose reductase inhibitors having antioxidant activity.
abstract: A series of aldose reductase (ALR2) inhibitors based on pyridothiadiazine were prepared and evaluated for their activities in ALR2 inhibition, DPPH scavenging, and MDA inhibition. Comparison studies were carried out between analogs having either hydroxyl or methoxy groups substituted on the N2-benzyl side chains of the compounds. Most of the hydroxy-substituted compounds were found to be more potent compared to their methoxy-substituted analogs with respect to DPPH inhibition (>93%) and MDA inhibition (>73%). However, ALR2 inhibitory activity was found to be affected by the electron-withdrawing substituent at the C7 position in addition to the effect of the N2-substituted benzyl group. These results provide an array of multifunctional ALR2 inhibitors possessing capacities both for ALR2 inhibition and as antioxidants.
authors.affiliation: a Department of Applied Chemistry , Beijing Institute of Technology , Beijing , China.
authors.forename: Shaojuan
authors.initials: S
authors.lastname: Zhu
authors.affiliation: a Department of Applied Chemistry , Beijing Institute of Technology , Beijing , China.
authors.forename: Shuzhen
authors.initials: S
authors.lastname: Zhang
authors.affiliation: a Department of Applied Chemistry , Beijing Institute of Technology , Beijing , China.
authors.forename: Xin
authors.initials: X
authors.lastname: Hao
authors.affiliation: a Department of Applied Chemistry , Beijing Institute of Technology , Beijing , China.
authors.forename: Xiangyu
authors.initials: X
authors.lastname: Qin
authors.affiliation: a Department of Applied Chemistry , Beijing Institute of Technology , Beijing , China.
authors.forename: Shagufta
authors.initials: S
authors.lastname: Parveen
authors.affiliation: a Department of Applied Chemistry , Beijing Institute of Technology , Beijing , China.
authors.forename: Shaoqi
authors.initials: S
authors.lastname: Yang
authors.affiliation: a Department of Applied Chemistry , Beijing Institute of Technology , Beijing , China.
authors.forename: Bing
authors.initials: B
authors.lastname: Ma
authors.affiliation: a Department of Applied Chemistry , Beijing Institute of Technology , Beijing , China.
authors.forename: Changjin
authors.initials: C
authors.lastname: Zhu
mesh_terms: D000449:Aldehyde Reductase / Q000037:antagonists & inhibitors* / Q000378:metabolism; D000975:Antioxidants / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology*; D004305:Dose-Response Relationship, Drug; D004791:Enzyme Inhibitors / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology*; D006801:Humans; D062105:Molecular Docking Simulation; D015394:Molecular Structure; D013329:Structure-Activity Relationship; D013829:Thiadiazines / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology*
chemical_list: D000975:Antioxidants; D004791:Enzyme Inhibitors; D013829:Thiadiazines; D000449:Aldehyde Reductase
keywords: Aldose reductase inhibitors; antioxidant activity; pyridothiadiazine derivatives; structure-activity relationships