790-04-5Relevant articles and documents
Synthesis of 2-iminothiazolidin-4-ones using guanine functionalized SBA-16 as a solid base catalyst
Gupta, Radha,Pathak, Devendra Deo
, (2021/11/08)
The first example of a one-pot three-component tandem annulation approach is described for the synthesis of 2-iminothiazolidin-4-ones by the reaction of aromatic/aliphatic amines, aryl isothiocyanates, and ethyl bromoacetate, catalysed by guanine-functionalized SBA-16, [SBA-16@G], as an efficient and recyclable heterogeneous solid base catalyst. The methodology is simple and offers a broad-substrate scope under mild reaction conditions.
Visible Light-Promoted Three-Component Tandem Annulation for the Synthesis of 2-Iminothiazolidin-4-ones
Guo, Wei,Zhao, Mingming,Tan, Wen,Zheng, Lvyin,Tao, Kailiang,Liu, Lingxiu,Wang, Xinyu,Chen, Deliang,Fan, Xiaolin
, p. 1402 - 1413 (2018/02/10)
Described is a visible light-promoted three-component tandem annulation of amines, aryl/alkyl isothiocyanates, and α-bromoesters to form 2-iminothiazolidin-4-ones in the absence of metal and photocatalyst at room temperature. This [1 + 2 + 2] cyclization strategy involves visible light-promoted C-S/C-N bond formation and features a powerful approach to the synthesis of 2-iminothiazolidin-4-ones with broad substrate scope, excellent functional group tolerance, mild reaction conditions, step-economy, and simple operation, which also has potential applications in the pharmaceutical industry. UV-vis spectroscopy indicates that an in situ-generated H-bonding electron donor-acceptor (EDA) complex probably acts as the photocatalyst, facilitating the reaction process.
Novel non-peptidic small molecule inhibitors of secreted aspartic protease 2 (SAP2) for the treatment of resistant fungal infections
Dong, Guoqiang,Liu, Yang,Wu, Ying,Tu, Jie,Chen, Shuqiang,Liu, Na,Sheng, Chunquan
, p. 13535 - 13538 (2019/01/05)
Targeting secreted aspartic protease 2 (SAP2), a kind of virulence factor, represents a new strategy for antifungal drug discovery. In this report, the first-generation of small molecule SAP2 inhibitors was rationally designed and optimized using a structure-based approach. In particular, inhibitor 23h was highly potent and selective and showed good antifungal potency for the treatment of resistant Candida albicans infections.