23023-16-7Relevant articles and documents
Catalytic asymmetric addition of dialkylzinc to 3,4-dihydroisoquinoline N-oxides utilizing tartaric acid ester as a chiral auxiliary
Ukaji, Yutaka,Shimizu, Yuuko,Kenmoku, Yuuichi,Ahmed, Alauddin,Inomata, Katsuhiko
, p. 447 - 452 (2000)
The catalytic asymmetric addition of dialkylzinc to a carbon-nitrogen double bond in 3,4-dihydroisoquinoline N-oxides was achieved by utilizing a catalytic amount of 2-magnesium 3-zinc salt of dicyclopentyl (R,R)-tartrate to afford (S)-1-alkyl-2-hydroxy-1
Discovery of Conformationally Restricted Human Glutaminyl Cyclase Inhibitors as Potent Anti-Alzheimer's Agents by Structure-Based Design
Hoang, Van-Hai,Ngo, Van T.H.,Cui, Minghua,Manh, Nguyen Van,Tran, Phuong-Thao,Ann, Jihyae,Ha, Hee-Jin,Kim, Hee,Choi, Kwanghyun,Kim, Young-Ho,Chang, Hyerim,MacAlino, Stephani Joy Y.,Lee, Jiyoun,Choi, Sun
, p. 8011 - 8027 (2019/10/11)
Alzheimer's disease (AD) is an incurable, progressive neurodegenerative disease whose pathogenesis cannot be defined by one single element but consists of various factors; thus, there is a call for alternative approaches to tackle the multifaceted aspects of AD. Among the potential alternative targets, we aim to focus on glutaminyl cyclase (QC), which reduces the toxic pyroform of β-amyloid in the brains of AD patients. On the basis of a putative active conformation of the prototype inhibitor 1, a series of N-substituted thiourea, urea, and α-substituted amide derivatives were developed. The structure-activity relationship analyses indicated that conformationally restrained inhibitors demonstrated much improved QC inhibition in vitro compared to nonrestricted analogues, and several selected compounds demonstrated desirable therapeutic activity in an AD mouse model. The conformational analysis of a representative inhibitor indicated that the inhibitor appeared to maintain the Z-E conformation at the active site, as it is critical for its potent activity.
A tandem annulation with a [1,3]-hydride transfer as the key step leading to isochromans
Wang, Yingwei,Li, Guangxun,Liu, Hongxin,Tang, Zhuo,Cao, Yuan,Zhao, Gang
supporting information, p. 10652 - 10655 (2017/10/06)
An unprecedented method that enables the direct coupling of an α-C-H bond in alcohols with 2-arylacetaldehydes through a [1,3]-hydride transfer ([1,3]-HT) of oxocarbenium ions catalyzed by a Lewis acid has been developed. The redox neutral preparation of