108124-77-2Relevant academic research and scientific papers
Targeting fungal virulence factor by small molecules: Structure-based discovery of novel secreted aspartic protease 2 (SAP2) inhibitors
Dong, Guoqiang,Han, Guiyan,Li, Chenglan,Liu, Na,Liu, Yang,Sheng, Chunquan,Tu, Jie,Wu, Shanchao
supporting information, (2020/07/06)
Secreted aspartic protease 2 (SAP2), a kind of virulence factor, is an emerging new antifungal target. Using docking-based virtual screening and structure-based inhibitor design, a series of novel SAP2 inhibitors were successfully identified. Among them, indolone derivative 24a showed potent SAP2 inhibitory activity (IC50 = 0.92 μM). It blocked fungi biofilm and hypha formation by down-regulating the expression of genes SAP2, ECE1, ALS3 and EFG1. As a virulence factor inhibitor, compound 24a was inactive in vitro and showed potent in vivo efficacy in a murine model of invasive candidiasis. It represents a promising lead compound for the discovery of novel antifungal agents.
Asymmetric synthesis of atropisomeric pyrazole: Via an enantioselective reaction of azonaphthalene with pyrazolone
Yuan, Huijun,Li, Yao,Zhao, Hanhui,Yang, Zhihong,Li, Xin,Li, Wenjun
supporting information, p. 12715 - 12718 (2019/10/28)
The first catalytic asymmetric reaction of azonaphthalene with pyrazolone has been established. A wide range of axially chiral pyrazole derivatives have been achieved in good yields (68-99%) with excellent enantioselectivities (83-98% ee) by utilizing chiral phosphoric acid as a catalyst. This strategy provides an efficient and facile approach for the construction of axially chiral pyrazole derivatives. Theoretical calculations were carried out to elucidate the origins of enantioselectivity.
Asymmetric [3 + 3] Annulation of Copper-Allenylidenes with Pyrazolones: Synthesis of Chiral 1,4-Dihydropyrano[2,3- c]pyrazoles
Jiang, Feng,Feng, Xinping,Wang, Rou,Gao, Xing,Jia, Hao,Xiao, Yumei,Zhang, Cheng,Guo, Hongchao
supporting information, p. 5278 - 5281 (2018/09/13)
The copper-catalyzed asymmetric [3 + 3] annulation of ethynyl benzoxazinanones with pyrazolones has been achieved, providing simple access to 1,4-dihydropyrano[2,3-c]pyrazole derivatives in moderate to excellent yields with excellent enantioselectivities (up to 99% ee). Compared with previous annulation reactions of copper-allenylidenes from ethynyl benzoxazinanones, the current reaction fused the three carbon atoms of the propargyl moiety into a heterocyclic framework.
Synthesis and evaluation of pyrazolone compounds as SARS-coronavirus 3C-like protease inhibitors
Ramajayam,Tan, Kian-Pin,Liu, Hun-Ge,Liang, Po-Huang
experimental part, p. 7849 - 7854 (2011/02/23)
A series of pyrazolone compounds as possible SARS-CoV 3CL protease inhibitors were designed, synthesized, and evaluated by in vitro protease assay using fluorogenic substrate peptide in which several showed potent inhibition against the 3CL protease. Interestingly, one of the inhibitors was also active against 3C protease from coxsackievirus B3. These inhibitors could be potentially developed into anti-coronaviral and anti-picornaviral agents.
