
Journal of Molecular Structure (2021)
Update date:2022-08-03
Topics:
Akhtar, Md Jawaid
Debnath, Biplab
Grover, Gourav
Nath, Rajarshi
Pathania, Shelly
Shahar Yar, M.
A series of N-(substituted benzothiazole-2-yl)-2-(2,3-dioxoindolin-1-yl)acetamide (4a-i) and substituted-[3-((5-phenyl-1,3,4-oxadiazole-2-yl)imino)indolene-2-one] (5a-f) were designed, synthesized fulfilling the structural requirement of pharmacophore and evaluated for anticonvulsant activities using maximal electroshock test (MES), subcutaneous pentylenetetrazole (scPTZ) seizures and neurotoxicity by motor impairment model in mice. The most active compoundN-(5-chlorobenzo[d]thiazol-2-yl)-2-(2,3-dioxoindolin-1-yl)acetamide (4a) has shown significant anticonvulsant activity against both MES and scPTZ screens and emerged as most effective anticonvulsant compound with median dose of 35.7 mg/kg (MES ED50), 88.15 mg/kg (scPTZ ED50) and toxic dose (TD50) was found to be > 500mg/kg. In silico studies including molecular docking study was carried to establish the molecular interaction of potent compound (4a) in both Na+ channel and GABAA receptors. The prediction of pharmacokinetic parameters and distance mapping of compounds were also performed to establish the drug likeness property.
View MoreSHANGHAI RC CHEMICALS CO.,LTD.
website:http://www.rcc.net.cn
Contact:+86-21-50322175
Address:Rm1415 Yinqiao Masion No.58 Jinxin Road Pudong Shanghai China
Shanghai Forever Biotech Co., Ltd.
Contact:+86-21-69734790
Address:Room 5017/5019、5022、5024 of Technology Innovation Centre, No.1155, Gongyuan East Rd, QingPu District, Shanghai China.
Shanghai Hongbang Medical Technology CO.,. Ltd
Contact:13671516988 /18917636693
Address:Room1, No67 Building, Yongde Road369, Wujing Town, Minhang Districy, Shanghai CIty, China.
Contact:86-551-63540590
Address:No 1388 Furong Rd., Hefei, Anhui, China
CHANGYI CITY FENGRUN FINE CHEMICAL CO.,LTD
website:http://www.fengrunhuagong.com
Contact:+86-536-7869976
Address:Changyi Coastal Economic Development Zone
Doi:10.1021/ja00345a044
(1983)Doi:10.1023/B:RUCB.0000046246.04868.88
(2004)Doi:10.1002/hlca.19860690524
(1986)Doi:10.1016/j.bmcl.2004.11.060
(2005)Doi:10.1016/j.jorganchem.2012.10.003
(2013)Doi:10.1016/j.cplett.2004.12.112
(2005)