Journal of Medicinal Chemistry p. 263 - 266 (1987)
Update date:2022-07-30
Topics:
White, R.L.
Wessels, F.L.
Schwan, T.J.
Ellis, K.O.
A series of 1-<<<5-(substituted phenyl)-2-oxazolyl>methylene>amino>-2,4-imidazolidinediones (6a-t) was synthesized, and the compounds were evaluated for direct skeletal muscle inhibition in the pithed rat gastrocnemius muscle preparation.The correctness of structural assignment of the new series was verified by alternate, unequivocal synthesis of one representative structure (6f).The phenyloxazoles 6d, 6g, 6j, 6k,and 6l exhibited significant skeletal muscle relaxant activity when administered intravenously and orally.The skeletal muscle relaxant effect of these five compounds is similar to that of other direct-acting skeletal muscle relaxants.The oxazole moiety proved to be an acceptable isosteric replacement for furan, as the biological activity in the oxazole series was retained.The synthesis of this new class of compounds is described, and pharmacologic evaluation data are presented.A discussion of structure-activity relationships is also presented.
View MoreShandong Zhongcheng Barium Salt Co., Ltd
Contact:+86-15725732638
Address:No.29 baoxi road, hi-tech zone, zibo, shandong
Beijing Greenchem Technology Co.,Ltd. ( Panjin Greenchem Technology Co.Ltd .)
website:http://www.bjgreenchem.com/
Contact:+86-427-6515887
Address:301,302, 3rd Floor, Building C-7, Dongsheng Science Park, Northern Territory, Zhongguancun, No. 66, Xixiaokou Road, Haidian District, Beijing
Frapp's Chemical (NFTZ) Co.,Ltd
Contact:+86-576-86137892
Address:General Chamber of Commercial Building, 159 Wanchang Middle Road, Wenling, Zhejiang, China
Contact:+86-13914766747
Address:Floors 21&22, Jin Cheng Tower, No. 216 Middle Longpan Road, Nanjing
Suzhou Sinosun Imp.&Exp. Corporation
website:http://www.szsinosun.com
Contact:+86-512-63488895,63488616
Address:No.758 East Jiangling Road Wujiang Economic & Technological Developmenty Zone Jiangsu China
Doi:10.1517/13543776.2011.548322
(2011)Doi:10.1021/ja01198a067
(1947)Doi:10.1002/jhet.5570450422
(2008)Doi:10.1016/j.jorganchem.2010.02.007
(2010)Doi:10.1002/ardp.19933260906
(1993)Doi:10.1080/00397919708007288
(1997)