European Journal of Medicinal Chemistry p. 300 - 307 (2016)
Update date:2022-08-17
Topics:
Roselli, Mariagrazia
Carocci, Alessia
Budriesi, Roberta
Micucci, Matteo
Toma, Maddalena
Di Cesare Mannelli, Lorenzo
Lovece, Angelo
Catalano, Alessia
Cavalluzzi, Maria Maddalena
Bruno, Claudio
De Palma, Annalisa
Contino, Marialessandra
Perrone, Maria Grazia
Colabufo, Nicola Antonio
Chiarini, Alberto
Franchini, Carlo
Ghelardini, Carla
Habtemariam, Solomon
Lentini, Giovanni
Four mexiletine analogues have been tested for their antiarrhythmic, inotropic, and chronotropic effects on isolated Guinea pig heart tissues and to assess calcium antagonist activity, in comparison with the parent compound mexiletine. All analogues showed from moderate to high antiarrhythmic activity. In particular, three of them (1b,c,e) were more active and potent than the reference drug, while exhibiting only modest or no negative inotropic and chronotropic effects and vasorelaxant activity, thus showing high selectivity of action. All compounds showed no cytotoxicity and 1b,c,d did not impair motor coordination. All in, these new analogues exhibit an interesting cardiovascular profile and deserve further investigation.
View MoreDayang Chem (Hangzhou) Co.,Ltd.
website:http://www.dycnchem.com
Contact:+86-571-88938639
Address:9/F, Unit 2 Changdi Torch Building, 259# WenSan Road, Xihu District, Hangzhou City 310012, P.R.China
Chiral Quest (Suzhou) Company Ltd
website:http://www.chiralquest.com
Contact:+86-0512-62956066
Address:B1/9, 218 Xinghu Street, Suzhou Industrial Park
Huangshan Honghui Pharm Technology Co., Ltd.
website:http://www.honghuichem.com
Contact:18855958372
Address:Qingshan Wan No.1,Nanyuan Kou,SheXian Huangshan City,Anhui Province
Wuhan Better Organic Technology Inc.
Contact:13307163183
Address:Wuhan Economic&Technology Development Zone, Hubei
website:https://www.bocsci.com/
Contact:1-631-485-4226
Address:Ramsey Road
Doi:10.1021/ja00884a019
(1963)Doi:10.1039/C39740000931
(1974)Doi:10.1021/ja00354a030
(1983)Doi:10.1055/s-1982-29916
(1982)Doi:10.1007/BF00632795
()Doi:10.1080/00958972.2014.982111
(2015)