Methods of treating disorders using compounds that modulate striatal-enriched tyrosine phosphatase (STEP) are described herein. Exemplary disorders include schizophrenia and cognitive deficit.
Photoredox-Promoted Selective Synthesis of C-5 Thiolated 2-Aminothiazoles from Terminal Alkynes
作者:Majid Ahmad Ganie、Muneer-ul-Shafi Bhat、Masood Ahmad Rizvi、Shabnam Raheem、Bhahwal Ali Shah
DOI:10.1021/acs.orglett.2c03064
日期:2022.10.28
A mild photoredox approach enabling the first one-step synthesis of thiolated 2-aminothiazoles has been reported. Notably, the incorporation of thio group on electron-rich heteroarenes such as aminothiazoles via conventional nucleophilic aromatic substitution (SNAr) presents a significant challenge owing to polarity mismatch. Herein, we present a remarkable site-selective installation of thio group
据报道,一种温和的光氧化还原方法能够首次一步合成硫醇化 2-氨基噻唑。值得注意的是,由于极性不匹配,通过传统的亲核芳香取代 (S N Ar)在富电子杂芳烃如氨基噻唑上并入硫代基团提出了重大挑战。在此,我们在富电子氨基噻唑骨架的 C-5 位置展示了一个显着的硫基位点选择性安装,并成功地将它们用于药物和天然产物的后功能化。
INDOLINE AND TETRAHYDROQUINOLINE SULFONYL INHIBITORS OF DIMETALLOENZYMES AND USE OF THE SAME
申请人:LOYOLA UNIVERSITY OF CHICAGO
公开号:US20190084932A1
公开(公告)日:2019-03-21
Indoline and tetrahydroquinoline sulfonyl compounds that can inhibit DapE and/or bacterial metallo-62 -lactamases (“MBLs”), such as NDM-1 are disclosed. Also disclosed are methods of treating an individual suffering from a bacterial infection using the compounds disclosed herein.