Bioorganic and Medicinal Chemistry Letters p. 2519 - 2525 (2004)
Update date:2022-09-26
Topics:
Chern, Jyh-Haur
Shia, Kak-Shan
Hsu, Tsu-An
Tai, Chia-Liang
Lee, Chung-Chi
Lee, Yen-Chun
Chang, Chih-Shiang
Tseng, Sung-Nien
Shih, Shin-Ru
A series of pyrazolo[3,4-d]pyrimidines were synthesized and their antiviral activity was evaluated in a plaque reduction assay. It is very interesting that this class of compounds provide remarkable evidence that they are very specific for human enteroviruses, in particular, coxsackieviruses. Some derivatives proved to be highly effective in inhibiting enterovirus replication at nanomolar concentrations. SAR studies revealed that the phenyl group at the N-1 position and the hydrophobic diarylmethyl group at the piperazine largely influenced the in vitro antienteroviral activity of this new class of potent antiviral agents. It was found that the pyrazolo[3,4-d]pyrimidines with a thiophene substituent, such as compounds 20-24, in general exhibited high activity against coxsackievirus B3 (IC50=0.063-0.089μM) and moderate activity against enterovirus 71 (IC50=0.32-0.65μM) with no apparent cytotoxic effect toward RD (rhabdomyosarcoma) cell lines (CC5025μ M).
View MoreContact:86-310-8067016
Address:East Fuhua Road,Tiexi Chemical Industrial Estate,Hebei,China
Shandong Zhongcheng Barium Salt Co., Ltd
Contact:+86-15725732638
Address:No.29 baoxi road, hi-tech zone, zibo, shandong
Hangzhou LINGEBA Technology Co., Ltd.
Contact:+0086-571-87389059
Address:Office 1-913,NewYouth Plaza, GongShu Area, HangZhou,ZheJiang,P.R.China
Shanghai Hanhong Scientific Co.,Ltd.
website:http://www.chemvia.com
Contact:+86-21-64541543,54280654,13918533501
Address:Jiachuan Road 245
Suzhou Wedo Chemicals Co., Ltd.
Contact:86 512 58100425
Address:Zonger Road, DongSha Industry Park , Zhangjiagang, Jiangsu, China
Doi:10.1021/ja9093583
(2010)Doi:10.1002/pola.27054
(2014)Doi:10.1016/S0040-4039(00)84824-8
(1986)Doi:10.1016/S0040-4039(00)80798-4
(1988)Doi:10.1039/b911951e
(2009)Doi:10.3184/030823409X12506792542783
(2009)