Synthesis and highly potent hypolipidemic activity of alpha-asarone- and fibrate-based 2-acyl and 2-alkyl phenols as HMG-CoA reductase inhibitors
作者:Aarón Mendieta、Fabiola Jiménez、Leticia Garduño-Siciliano、Angélica Mojica-Villegas、Blanca Rosales-Acosta、Lourdes Villa-Tanaca、Germán Chamorro-Cevallos、José L. Medina-Franco、Nathalie Meurice、Rsuini U. Gutiérrez、Luisa E. Montiel、María del Carmen Cruz、Joaquín Tamariz
DOI:10.1016/j.bmc.2014.09.022
日期:2014.11
In the search for new potential hypolipidemic agents, the present study focused on the synthesis of 2-acyl phenols (6a–c and 7a–c) and their saturated side-chain alkyl phenols (4a–c and 5a–c), and on the evaluation of their hypolipidemic activity using a murine Tyloxapol-induced hyperlipidemic protocol. The whole series of compounds 4–7 greatly and significantly reduced elevated serum levels of total
Identification and SAR of novel diaminopyrimidines. Part 1: The discovery of RO-4, a dual P2X3/P2X2/3 antagonist for the treatment of pain
作者:David S. Carter、Muzaffar Alam、Haiying Cai、Michael P. Dillon、Anthony P.D.W. Ford、Joel R. Gever、Alam Jahangir、Clara Lin、Amy G. Moore、Paul J. Wagner、Yansheng Zhai
DOI:10.1016/j.bmcl.2009.02.003
日期:2009.3
P2X purinoceptors are ligand-gated ion channels whose endogenous ligand is ATP. Both the P2X(3) and P2X(2/3) receptor subtypes have been shown to play an important role in the regulation of sensory function and dual P2X(3)/P2X(2/3) antagonists offer significant potential for the treatment of pain. A high-throughput screen of the Roche compound collection resulted in the identification of a novel series of diaminopyrimidines; subsequent optimization resulted in the discovery of RO-4, a potent, selective and drug-like dual P2X(3)/P2X(2/3) antagonist. (C) 2009 Elsevier Ltd. All rights reserved.
Spaeth; Pailer; Gergely, Chemische Berichte, 1940, vol. 73, p. 935,937
作者:Spaeth、Pailer、Gergely
DOI:——
日期:——
Zur Konstitution des Emetins
作者:E. Sp�th、M. Pailer
DOI:10.1007/bf01090955
日期:1948.9
2-OXO-5H-CHROMENO[4,3-B]PYRIDINES FOR USE IN THE TREATMENT OF HEPATITIS B