86826-93-9Relevant articles and documents
Copper-Catalyzed Lactamization of (E)-2-(2-Bromophenyl)-3-arylacrylamides for the Synthesis of (E)-3-Arylideneindolin-2-ones
Luo, Xiang,Zhang, Qianzhong,Jiang, Yi,Wang, Chengxin,Song, Xianheng,Li, Jianheng,Yan, Qinfang,Chan, Albert S. C.,Zou, Yong
, p. 6698 - 6710 (2021/05/29)
A copper-catalyzed, ligand-free intramolecular C-N coupling of (E)-2-(2-bromophenyl)-3-arylacrylamides has been developed. This protocol provides an efficient and practical synthetic route for the biologically important (E)-3-arylideneindolin-2-ones from
INHIBITORS OF NOTCH SIGNALLING PATHWAY AND USE THEREOF IN TREATMENT OF CANCERS
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Page/Page column 124, (2020/10/21)
The present invention relates to new inhibitors of Notch signalling pathway and its use in the treatment and/or prevention of cancers.
Simple analogues of natural product chelerythrine: Discovery of a novel anticholinesterase 2-phenylisoquinolin-2-ium scaffold with excellent potency against acetylcholinesterase
Cui, Zhiming,Gao, Jinming,Geng, Huiling,Li, Ding,Li, Hui,Zhou, Bohang,Zhou, Le
, (2020/05/25)
As simple analogues of the natural compound chelerythrine, a novel anti-cholinesterase 2-phenylisoquinolin-2-ium scaffold was designed by structure imitation. The activity evaluation led to the discovery of seven compounds with potent anti-acetylcholinesterase activity with IC50 values of ≤0.72 μM, superior to chelerythrine and standard drugs galantamine. Particularly, compound 8y showed the excellent dual acetylcholinesterase-butyrylcholinesterase inhibition activity, superior to rivastigmine, a dual cholinesterase inhibitor drug. Furthermore, the compounds displayed a competitive anti-acetylcholinesterase mechanism with the substrate and low cytotoxicity. Molecular docking showed that the isoquinoline moiety is embedded in a cavity surrounded by four aromatic residues of acetylcholinesterase by the π-π action. Structure-activity relationship showed that the p-substituents on the C-ring can dramatically improve the anti-acetylcholinesterase activity, while 8-OMe can increase the activity against the two cholinesterases simultaneously. Thus, the title compounds emerged as promising lead compounds for the development of novel cholinesterase inhibitor agents.
N-SUBSTITUTED TETRAHYDROTHIENOPYRIDINE DERIVATIVES AND USES THEREOF
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Paragraph 00156; 00189, (2020/01/11)
A compound of Formula (I) is provided that has been shown to be useful for treating a disease caused by a viral infection: (I) wherein R1, R2, R3, A, L, m, n, p and q are as defined herein.
Chiral Magnesium Bisphosphate-Catalyzed Asymmetric Double C(sp3)-H Bond Functionalization Based on Sequential Hydride Shift/Cyclization Process
Mori, Keiji,Isogai, Ryo,Kamei, Yuto,Yamanaka, Masahiro,Akiyama, Takahiko
, p. 6203 - 6207 (2018/05/23)
Described herein is a chiral magnesium bisphosphate-catalyzed asymmetric double C(sp3)-H bond functionalization triggered by a sequential hydride shift/cyclization process. This reaction consists of stereoselective domino C(sp3)-H bond functionalization: (1) a highly enantio- and diastereoselective C(sp3)-H bond functionalization by chiral magnesium bisphosphate (first [1,5]-hydride shift), and (2) a highly diastereoselective C(sp3)-H bond functionalization by an achiral catalyst (Yb(OTf)3, second [1,5]-hydride shift).
Highly diastereoselective synthesis of tetralin-fused spirooxindoles via lewis acid-catalyzed C(sp3)H bond functionalization
Machida, Mizuki,Mori, Keiji
, p. 868 - 871 (2018/07/03)
A highly diastereoselective synthesis of tetralin-fused spirooxindole derivatives was described. Treatment of benzylidene oxindoles with a catalytic amount of Sc(OTf)3 in refluxing hexane afforded the target compounds in good chemical yields with excellent diastereoselectivities (up to >20:1). Detailed investigation of the reaction mechanism revealed that both interconversion of the two diastereomers and their solubility difference in reaction medium were the key to achieving excellent diastereoselectivities.
Synthesis, bioactivity and structure-activity relationships of new 2-aryl-8-OR-3,4-dihydroisoquinolin-2-iums salts as potential antifungal agents
Zhu, Li-Fei,Hou, Zhe,Zhou, Kun,Tong, Zong-Bo,Kuang, Qian,Geng, Hui-Ling,Zhou, Le
, p. 2413 - 2417 (2016/07/07)
As our continuing research on antifungal dihydroisoquinolin-2-ium salts, forty 2-aryl-8-OR-3,4-dihydroisoquinolin-2-ium bromides were synthesized and characterized by spectroscopic analysis. By using the mycelium growth rate method, the compounds were evaluated for antifungal activity against three plant pathogenic fungi and structure-activity relationships (SAR) were derived. The vast majority of the compounds displayed the medium to high activity with inhibition rates of 50-100% at 150 μM. About half of the compounds were more active than their natural model compounds sanguinarine and chelerythrine for all the fungi, and part or most of them were more active than positive drugs thiabendazole and azoxystrobin. SAR analysis showed that both substitution patterns of the C-ring and the type of 8-OR group significantly influenced the activity. Thus, a series of new title compounds with excellent antifungal potency emerged.
Total synthesis of (-)-Haouamine B pentaacetate and structural revision of haouamine B
Momoi, Yuichi,Okuyama, Kei-Ichiro,Toya, Hiroki,Sugimoto, Kenji,Okano, Kentaro,Tokuyama, Hidetoshi
supporting information, p. 13215 - 13219 (2015/01/09)
The enantiocontrolled total synthesis of (-)-haouamine B pentaacetate was accomplished via an optically active indane-fused β-lactam, which was prepared by a newly developed Friedel-Crafts reaction. Subsequent cleavage of the β-lactam and an intramolecular McMurry coupling reaction provided the core indane-fused tetrahydropyridine, which led to the elucidation of the structure, as proposed by Trauner and Zuba.
SPIRO-AMINO-IMIDAZOLONE AND SPIRO-AMINO-DIHYDRO-PYRIMIDINONE COMPOUNDS AS BETA-SECRETASE MODULATORS AND METHODS OF USE
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Page/Page column 68, (2012/06/15)
The present invention provides a new class of compounds useful for the modulation of beta-secretase enzyme (BACE) activity. The compounds have a general Formula (I), wherein variables A1, A3, A4, A5, A6/su
Synthesis of N-alkoxyindol-2-ones by copper-catalyzed intramolecular N-arylation of hydroxamates
Kukosha, Tatyana,Trufilkina, Nadezhda,Katkevics, Martins
, p. 2525 - 2528 (2011/11/13)
The first example of copper-catalyzed intramolecular N-arylation of hydroxamic acid derivatives is presented. Based on this transformation a new method for the synthesis of N-alkoxyindol-2-ones from 2-(2-bromoaryl) acetylhydroxamates has been developed. T