22283-43-8Relevant articles and documents
Discovery of Multitarget Agents Active as Broad-Spectrum Antivirals and Correctors of Cystic Fibrosis Transmembrane Conductance Regulator for Associated Pulmonary Diseases
Tassini, Sabrina,Sun, Liang,Lanko, Kristina,Crespan, Emmanuele,Langron, Emily,Falchi, Federico,Kissova, Miroslava,Armijos-Rivera, Jorge I.,Delang, Leen,Mirabelli, Carmen,Neyts, Johan,Pieroni, Marco,Cavalli, Andrea,Costantino, Gabriele,Maga, Giovanni,Vergani, Paola,Leyssen, Pieter,Radi, Marco
, p. 1400 - 1416 (2017/03/08)
Enteroviruses (EVs) are among the most frequent infectious agents in humans worldwide and represent the leading cause of upper respiratory tract infections. No drugs for the treatment of EV infections are currently available. Recent studies have also linked EV infection with pulmonary exacerbations, especially in cystic fibrosis (CF) patients, and the importance of this link is probably underestimated. The aim of this work was to develop a new class of multitarget agents active both as broad-spectrum antivirals and as correctors of the F508del-cystic fibrosis transmembrane conductance regulator (CFTR) folding defect responsible for >90% of CF cases. We report herein the discovery of the first small molecules able to simultaneously act as correctors of the F508del-CFTR folding defect and as broad-spectrum antivirals against a panel of EVs representative of all major species.
Aminothiazole compound, and preparation method and application thereof
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Paragraph 0045; 0046; 0047, (2016/10/08)
The invention discloses an aminothiazole compound, and a preparation method and an application thereof. The compound has a following structural formula. In the formula, n, m, x are all 0 or 1, and only one of the three is 1 or the three are 0 at a same time; R1 is hydrogen, 2-pyridyl, 3-pyridyl, 4-pyridyl, phenyl, 2-pyrazinyl, 2-furyl, 2-thienyl, 2-pyrrolyl, 2-quinolyl, or 2-methylenepyridine; R2 is hydrogen or alkane with 1-10 aliphatic carbon chains; R3 or R4 is hydrogen or as the picture; R5 is hydrogen, a structure as the picture, N,N-diethyl, N,N-dipropyl, methyl, ethyl, propyl, butyl, trifluoromethyl, methoxy or cyano; among R3, R4 and R5, two are hydrogen at a same time; R6 and R7 can be same or different, and can be H, alkane with 1-10 aliphatic carbon chains, olefin or alkyne. In animal bodies, the compounds can inhibit the proliferation and growth of KRAS high mutant tumors such as pancreatic cancer and colon cancer.
Synthesis of thiophene-2-carboxamidines containing 2-aminothiazoles and their biological evaluation as urokinase inhibitors
Wilson, Kenneth J.,Illig, Carl R.,Subasinghe, Nalin,Hoffman, James B.,Jonathan Rudolph,Soll, Richard,Molloy, Christopher J.,Bone, Roger,Green, David,Randall, Troy,Zhang, Marie,Lewandowski, Frank A.,Zhou, Zhao,Sharp, Celia,Maguire, Diane,Grasberger, Bruce,DesJarlais, Renee L.,Spurlino, John
, p. 915 - 918 (2007/10/03)
The serine protease urokinase (uPa) has been implicated in the progression of both breast and prostate cancer. Utilizing structure based design, the synthesis of a series of substituted 4-[2-amino-1,3-thiazolyl]-thiophene-2-carboxamidines is described. Further optimization of this series by substitution of the terminal amine yielded urokinase inhibitors with excellent activities.