title: Design, synthesis and evaluation of the antidepressant and anticonvulsant activities of triazole-containing quinolinones.
abstract: A series of 1-substituted-6-(4H-1,2,4-triazol-4-yl)-3,4-dihydroquinolin-2(1H)-ones were designed, synthesized, and screened for their antidepressant and anticonvulsant activities. Interestingly, compounds 5i, 5j, 5m, and 5n led to significant reductions in the immobility time in the forced swimming test at a dose of 50 mg/kg, and exhibited higher levels of efficacy than the reference standard fluoxetine. In addition, compound 5i exhibited greater efficacy than fluoxetine in the tail suspension test. The results of an open field test further confirmed that compound 5i provided a good antidepressant effect. In the maximal electroshock seizure screen, compounds 5c and 5d showed moderate levels of anticonvulsant activity and protected 100% of the animals at a dose of 100 mg/kg. None of the synthesized compounds showed any neurotoxicity in the rotarod test at a dose of 100 mg/kg.
authors.affiliation: Medical College, Jinggangshan University, Ji'an, Jiangxi 343009, China.
authors.forename: Xian-Qing
authors.initials: XQ
authors.lastname: Deng
authors.affiliation: Medical College, Jinggangshan University, Ji'an, Jiangxi 343009, China.
authors.forename: Ming-Xia
authors.initials: MX
authors.lastname: Song
authors.affiliation: College of Pharmacy, Yanbian University, Yanji, Jilin 133002, China. Electronic address: yzheng@ybu.edu.cn.
authors.forename: Yan
authors.initials: Y
authors.lastname: Zheng
authors.affiliation: College of Pharmacy, Yanbian University, Yanji, Jilin 133002, China. Electronic address: zsquan@ybu.edu.cn.
authors.forename: Zhe-Shan
authors.initials: ZS
authors.lastname: Quan
mesh_terms: D000818:Animals; D000927:Anticonvulsants / Q000138:chemical synthesis* / Q000737:chemistry / Q000627:therapeutic use / Q000633:toxicity; D000928:Antidepressive Agents / Q000138:chemical synthesis* / Q000737:chemistry / Q000627:therapeutic use / Q000633:toxicity; D001522:Behavior, Animal / Q000187:drug effects; D004195:Disease Models, Animal; D004305:Dose-Response Relationship, Drug; D015195:Drug Design; D004597:Electroshock; D005106:Exploratory Behavior / Q000187:drug effects; D008297:Male; D051379:Mice; D008815:Mice, Inbred Strains; D015394:Molecular Structure; D015363:Quinolones / Q000138:chemical synthesis* / Q000737:chemistry / Q000627:therapeutic use / Q000633:toxicity; D045442:Rotarod Performance Test; D012640:Seizures / Q000188:drug therapy / Q000209:etiology; D013550:Swimming; D014230:Triazoles / Q000737:chemistry*
chemical_list: D000927:Anticonvulsants; D000928:Antidepressive Agents; D015363:Quinolones; D014230:Triazoles
keywords: Anticonvulsant; Antidepressant; Forced swimming test; Maximal electroshock seizure; Quinolinone; Triazole