STUDIES TOWARD IDENTIFYING THE PHARMACOPHORE OF L-755,807 FOR AMYLOID-β AGGREGATION INHIBITORY ACTIVITY

被引：1

作者：

Kobayashi, Kenichi ^{[1
]}

Tanaka, Kosaku, III ^{[1
]}

Honma, Yusuke ^{[1
]}

Suzuki, Momoko ^{[1
]}

Kogen, Hiroshi ^{[1
]}

机构：

[1] Meiji Pharmaceut Univ, Grad Sch Pharmaceut Sci, 2-522-1 Noshio, Tokyo 2048588, Japan

来源：

HETEROCYCLES | 2019年 / 98卷 / 12期

关键词：

L-755,807; Amyloid-p Aggregation Inhibitory Activity; Alzheimer's Disease; Epoxy-gamma-lactam; Pharmacophore; MECHANISTIC INSIGHTS; ALZHEIMERS-DISEASE; DERIVATIVES; OLIGOMERS; AGENTS;

D O I：

10.3987/COM-19-14193

中图分类号：

O62 [有机化学];

学科分类号：

070303 ; 081704 ;

摘要：

To investigate the structure activity relationship of L-755,807 for amyloid-beta aggregation inhibitory activity, L-755,807 analogs were synthesized and biologically evaluated. The results suggest that a hydrophobic conjugated carbon chain with a terminal hydrophilic functional group is essential for the potent activity. These findings provide a starting point for identifying the pharmacophore of L-755,807.

引用

页码：1769 / 1776

页数：8

共 9 条

[1] Total Synthesis and Amyloid β Aggregation Inhibitory Activity of (-)-L-755,807
Tanaka, Kosaku, III
Kobayashi, Kenichi
Kogen, Hiroshi
JOURNAL OF SYNTHETIC ORGANIC CHEMISTRY JAPAN, 2019, 77 (07) : 673 - 683
[2] Studies toward the total synthesis of L-755,807: A novel non-peptide bradykinin inhibitor.
Clark, AJ
Ellard, JM
ABSTRACTS OF PAPERS OF THE AMERICAN CHEMICAL SOCIETY, 1999, 218 : U186 - U186
[3] Experimental and theoretical studies toward the development of new amyloid inhibitors against amyloid-β aggregation
Zheng, Jie
ABSTRACTS OF PAPERS OF THE AMERICAN CHEMICAL SOCIETY, 2016, 251
[4] Cultivation Factors That Affect Amyloid-β Aggregation Inhibitory Activity in Perilla frutescens var. crispa
Shimamori, Keiya
Nambu, Tomohiko
Kawamata, Daiki
Kuragano, Masahiro
Nishishita, Naoki
Iimori, Toshifumi
Yamanaka, Shinya
Uwai, Koji
Tokuraku, Kiyotaka
FOODS, 2023, 12 (03)
[5] Inhibitory activity on amyloid-β aggregation and antioxidant properties of Crocus sativus stigmas extract and its crocin constituents
Papandreou, Magdalini A.
Kanakis, Charalambos D.
Polissiou, Moschos G.
Efthimiopoulos, Spyros
Cordopatis, Paul
Margarity, Marigoula
Lamari, Fotini N.
JOURNAL OF AGRICULTURAL AND FOOD CHEMISTRY, 2006, 54 (23) : 8762 - 8768
[6] Inhibitory Activity of Curcumin Derivatives Towards Metal-Free and Metal-Induced Amyloid-β Aggregation
Kochi, Akiko
Lee, Hyuck Jin
Vithanarachchi, Sashiprabha M.
Padmini, Vediappen
Allen, Matthew J.
Lim, Mi Hee
CURRENT ALZHEIMER RESEARCH, 2015, 12 (05) : 415 - 423
[7] Catechol-Type Flavonoids from the Branches of Elaeagnus glabra f. oxyphylla Exert Antioxidant Activity and an Inhibitory Effect on Amyloid-β Aggregation
Kim, Yu Jin
Sohn, Eunjin
Kim, Joo-Hwan
Na, MinKyun
Jeong, Soo-Jin
MOLECULES, 2020, 25 (21):
[8] Novel Huprine Derivatives with Inhibitory Activity toward β-Amyloid Aggregation and Formation as Disease-Modifying Anti-Alzheimer Drug Candidates
Viayna, Elisabet
Gomez, Tania
Galdeano, Carles
Ramirez, Lorena
Ratia, Miriam
Badia, Albert
Clos, M. Victoria
Verdaguer, Ester
Junyent, Felix
Camins, Antoni
Pallas, Merce
Bartolini, Manuela
Mancini, Francesca
Andrisano, Vincenza
Arce, Mariana P.
Rodriguez-Franco, Maria Isabel
Bidon-Chanal, Axel
Luque, F. Javier
Camps, Pelayo
Munoz-Torrero, Diego
CHEMMEDCHEM, 2010, 5 (11) : 1855 - 1870
[9] 2,4-Disubstituted quinazolines as amyloid-β aggregation inhibitors with dual cholinesterase inhibition and antioxidant properties: Development and structure-activity relationship (SAR) studies
Mohamed, Tarek
Rao, Praveen P. N.
EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY, 2017, 126 : 823 - 843

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