MedChemComm p. 1297 - 1302 (2017)
Update date:2022-08-05
Topics:
Zeng, Fanxun
Qi, Tiantian
Li, Chunyan
Li, Tingfang
Li, Honglin
Li, Shiliang
Zhu, Lili
Xu, Xiaoyong
A series of 4-thiazolidinone derivatives were synthesized and evaluated as novel human dihydroorotate dehydrogenase (hDHODH) inhibitors. Compounds 26 and 31 displayed IC50 values of 1.75 and 1.12 μM, respectively. The structure-activity relationship was summarized. Further binding mode analysis revealed that compound 31 could form a hydrogen bond with Tyr38 and a water-mediated hydrogen bond with Ala55, which may be necessary for maintaining the bioactivities of the compounds in this series. Further structural optimization of the para- or meta-position of the phenyl group at R will lead to the identification of more potent hDHODH inhibitors.
View MoreHangzhou Yanshan Chemical Co.,Ltd.
Contact:86-571- 87698076
Address:Room 1001, #1 Building, Zhongtian MCC, No.2 Youzhinong, Wenyi West Road, Xihu District, Hangzhou, China
Shanghai Sinofluoro Scientific Co., Ltd
Contact:+86-21-64279360
Address:Room 1006,Building 3,#58 East Xinjian Road, Shanghai ,201100,China,
WUHU HUAHAI BIOLOGY ENGINEERING CO LTD
Contact:+86-553-3836920
Address:7/F NO.82 LAODONG ROAD WUHU CHINA
Yancheng Creator Chemical Co., Ltd
Contact:0086-515-88710008 88710068 88710858 88710868
Address:No.21 Renming Road, Longgang Town, Yandu County,Yancheng City
Xiamen Huasing Chemicals Co.Ltd.
Contact:0086-592-6228397
Address:NO.24, Xinglin North 2nd Road,Jimei district
Doi:10.1016/j.bmc.2005.10.050
(2006)Doi:10.1021/om050897e
(2006)Doi:10.1055/s-2005-921907
(2005)Doi:10.1246/bcsj.78.2171
(2005)Doi:10.1021/ja00314a050
(1984)Doi:10.1021/ja983267v
(1999)