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.
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