1051934-79-2Relevant academic research and scientific papers
The optimization of a novel selective antagonist for human M2 muscarinic acetylcholine receptor
Li, Miaomiao,Huang, Chen,Wu, Xingyu,Ding, Fan,Hu, Zhoumi,Zhu, Yan,Zhao, Lanxue,Hou, Lina,Chen, Hongzhuan,Wang, Hao,Xu, Jianrong,Tang, Dewei
, (2020)
Muscarinic acetylcholine receptors (mAChRs) comprise five distinct subtypes denoted M1 to M5. The antagonism of M2 subtype could increase the release of acetylcholine from vesicles into the synaptic cleft and improve postsynaptic functions in the hippocampus via M1 receptor activation, displaying therapeutic potentials for Alzheimer's disease. However, drug development for M2 antagonists is still challenged among different receptor subtypes. In this study, by optimizing a scaffold from virtual screening, we synthesized two focused libraries and generated up to 50 derivatives. By measuring potency and binding selectivity, we discovered a novel M2 antagonist, ligand 47, featuring submicromolar IC50, high M2/M4 selectivity (~30-fold) and suitable lipophilicity (cLogP = 4.55). Further study with these compounds also illustrates the structure–activity relationship of this novel scaffold. Our study could not only provide novel lead structure, which was easy to synthesize, but also offer valuable information for further development of selective M2 ligands.
M2 acetylcholine receptor antagonist and use thereof
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Paragraph 0104-0106; 0139-0140, (2021/10/27)
The invention relates to an M2 acetylcholine receptor antagonist and use thereof. The invention relates to compounds having a structure as shown in a formula I. The compounds can be used as novel M2 acetylcholine receptor subtype selective antagonists and can be used for preparing medicines for treating Alzheimer's disease.
Synthesis and antimicrobial activities of novel tetrahydroquinoline and tetrahydroisoquinoline analogues
Ganguly, Swastika,Murugesan
experimental part, p. 879 - 885 (2011/04/25)
A series of tetrahydroquinoline and tetrahydroisoquinoline derivatives were synthesized and their structures were confirmed by spectral (FT-IR, NMR and Mass) data analysis. These analogs were evaluated for their in vitro antibacterial activity against Sta
