40107-06-0Relevant articles and documents
Repurposing human PDE4 inhibitors for neglected tropical diseases. evaluation of analogs of the human PDE4 inhibitor GSK-256066 as inhibitors of pdeb1 of trypanosoma brucei
Ochiana, Stefan O.,Bland, Nicholas D.,Settimo, Luca,Campbell, Robert K.,Pollastri, Michael P.
, p. 549 - 564 (2015/04/22)
Cyclic nucleotide phosphodiesterases (PDEs) have been identified as important enzyme targets for drug development in both humans and Trypanosoma brucei, the causative agent of human African trypanosomiasis. With this in mind, we recently reported the prof
C-6 aryl substituted 4-quinolone-3-carboxylic acids as inhibitors of hepatitis C virus
Chen, Yue-Lei,Zacharias, Jeana,Vince, Robert,Geraghty, Robert J.,Wang, Zhengqiang
, p. 4790 - 4800 (2012/08/28)
Quinolone-3-carboxylic acid represents a highly privileged chemotype in medicinal chemistry and has been extensively explored as antibiotics and antivirals targeting human immunodeficiency virus (HIV) integrase (IN). Herein we describe the synthesis and anti-hepatitis C virus (HCV) profile of a series of C-6 aryl substituted 4-quinlone-3-carboxylic acid analogues. Significant inhibition was observed with a few analogues at low micromolar range against HCV replicon in cell culture and a reduction in replicon RNA was confirmed through an RT-qPCR assay. Interestingly, evaluation of analogues as inhibitors of NS5B in a biochemical assay yielded only modest inhibitory activities, suggesting that a different mechanism of action could operate in cell culture.
IMAGING AGENTS
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Page/Page column 23-24, (2009/05/29)
The invention relates to compounds of formula (I), or a salt or solvate thereof which comprise a detectable label. The compounds have use as radioligands for the GABAA receptor.
Quinolines as a novel structural class of potent and selective PDE4 inhibitors. Optimisation for inhaled administration
Woodrow, Michael D.,Ballantine, Stuart P.,Barker, Michael D.,Clarke, Beth J.,Dawson, John,Dean, Tony W.,Delves, Christopher J.,Evans, Brian,Gough, Sharon L.,Guntrip, Steven B.,Holman, Stuart,Holmes, Duncan S.,Kranz, Michael,Lindvaal, Mika K.,Lucas, Fiona S.,Neu, Margarete,Ranshaw, Lisa E.,Solanke, Yemisi E.,Somers, Don O.,Ward, Peter,Wiseman, Joanne O.
scheme or table, p. 5261 - 5265 (2010/03/31)
Crystallography driven optimisation of a lead derived from similarity searching of the GSK compound collection resulted in the discovery of quinoline-3-carboxamides as highly potent and selective inhibitors of phosphodiesterase 4B. This series has been optimized to GSK256066, a potent PDE4B inhibitor which also inhibits LPS induced production of TNF-α from isolated human peripheral blood mononuclear cells with a pIC50 of 11.1. GSK256066 also has a suitable profile for inhaled dosing.
Controlled derivatization of polyhalogenated quinolines utilizing selective cross-coupling reactions
Brad Nolt,Zhao, Zhijian,Wolkenberg, Scott E.
, p. 3137 - 3141 (2008/09/20)
Straightforward procedures for the derivatization of tri- and tetrahalogenated quinolines utilizing sequential selective Pd-catalyzed cross-coupling reactions are described. Taking advantage of intrinsic halide reactivity, substrate control, and appropria
Evaluation of 3-carboxy-4(1H)-quinolones as inhibitors of human protein kinase CK2
Golub, Andriy G.,Yakovenko, Olexander Ya.,Bdzhola, Volodymyr G.,Sapelkin, Vladislav M.,Zien, Piotr,Yarmoluk, Sergiy M.
, p. 6443 - 6450 (2007/10/03)
Due to the emerging role of protein kinase CK2 as a molecule that participates not only in the development of some cancers but also in viral infections and inflammatory failures, small organic inhibitors of CK2, besides application in scientific research, may have therapeutic significance. In this paper, we present a new class of CK2 inhibitors-3-carboxy-4(1H)-quinolones. This class of inhibitors has been selected via receptor-based virtual screening of the Otava compound library. It was revealed that the most active compounds, 5,6,8-trichloro-4-oxo-1,4-dihydroquinoline-3-carboxylic acid (7) (IC 50 = 0.3 μM) and 4-oxo-1,4-dihydrobenzo[h]quinoline-3-carboxylic acid (9) (IC50 = 1 μM), are ATP competitive (Ki values are 0.06 and 0.28 μM, respectively). Evaluation of the inhibitors on seven protein kinases shows considerable selectivity toward CK2. According to theoretical calculations and experimental data, a structural model describing the key features of 3-carboxy-4(1H)-quinolones responsible for tight binding to CK2 active site has been developed.
4-HYDROXYQUINOLINE-3-CARBOXAMIDES AND HYDRAZIDES AS ANTIVIRAL AGENTS
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Page/Page column 77, (2010/02/13)
The present invention provides 4-hydroxyquinoline-3-carboxamide and hydrazide compounds of formula I These compounds are useful to treat or prevent the herpesviral infections, particularly, human cytomegaloviral infection.
NOVEL QUINOLINE DERIVATIVES
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Page/Page column 64, (2008/06/13)
The invention relates to compounds represented by Formula (I): and to pharmaceutically acceptable salts or solvates of said compounds, wherein each of A, R3-8, X3, X5, m, and n are defined herein. The invention also relates to pharmaceutical compositions containing the compounds of Formula (I) and to methods of treating hyperproliferative disorders in a mammal by administering compounds of Formula (I).
ESTER LINKED MACROLIDES USEFUL FOR THE TREATMENT OF MICROBIAL INFECTIONS
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Page/Page column 77-78, (2008/06/13)
The present invention relates to 14- or 15-membered macrolides substituted at the 4” position of formula (I) and pharmaceutically acceptable derivatives thereof, to processes for their preparation and their use in therapy or prophylaxis of systemic or top
DERIVATIVES OF 3-AMINOCARBONYLQUINOLINE, PHARMACEUTICAL COMPOSITIONS CONTAINING THEM AND PROCESSES AND INTERMEDIATES FOR THEIR PREPARATION
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Page/Page column 36, (2008/06/13)
Compounds of formula (I) or pharmaceutically acceptable salts thereof are inhibitors of phosphodiesterase type IV (PDE4) and are of use in the treatment of inflammatory and/or allergic diseases.
