Biological activity of modified and exchanged 2-amino-5-nitrothiazole amide analogues of nitazoxanide
作者:T. Eric Ballard、Xia Wang、Igor Olekhnovich、Taylor Koerner、Craig Seymour、Paul S. Hoffman、Timothy L. Macdonald
DOI:10.1016/j.bmcl.2010.04.126
日期:2010.6
Head group analogues of the antibacterial and antiparasitic drug nitazoxanide (NTZ) are presented. A library of 39 analogues was synthesized and assayed for their ability to suppress growth of Helicobacter pylori, Campylobacter jejuni, Clostridium difficile and inhibit NTZ target pyruvate: ferredoxin oxidoreductase (PFOR). Two head groups assayed recapitulated NTZ activity and possessed improved activity over their 2-amino-5-nitrothiazole counterparts, demonstrating that head group modification is a viable route for the synthesis of NTZ-related antibacterial analogues. (C) 2010 Elsevier Ltd. All rights reserved.
KRAVCHENYA, N. A, XIM.-FARMATS. ZH., 1983, 17, N 8, 975-977
作者:KRAVCHENYA, N. A
DOI:——
日期:——
GLUCOKINASE ACTIVATORS
申请人:Takeda San Diego, Inc.
公开号:EP2091947A2
公开(公告)日:2009-08-26
[EN] GLUCOKINASE ACTIVATORS<br/>[FR] ACTIVATEURS DE GLUCOKINASE
申请人:TAKEDA SAN DIEGO INC
公开号:WO2008079787A2
公开(公告)日:2008-07-03
(EN) Compounds of the following formula are provided for use with glucokinase: Formula (I), wherein the variables are as defined herein. Also provided are pharmaceutical compositions, kits and articles of manufacture comprising such compounds; methods and intermediates useful for making the compounds; and methods of using said compounds.(FR) L'invention concerne des composés représentés par la formule suivante destinés à une utilisation avec une glucokinase. Les variables sont telles que définies dans les spécifications. L'invention concerne aussi des compositions pharmaceutiques, des kits et des articles de manufacture comprenant ces composés, des procédés et des intermédiaires qui conviennent pour la fabrication de ces composés et des procédés d'utilisation de ces composés.