205037-64-5Relevant articles and documents
Structure-based design, synthesis, and SAR evaluation of a new series of 8-hydroxyquinolines as HIF-1α prolyl hydroxylase inhibitors
Warshakoon, Namal C.,Wu, Shengde,Boyer, Angelique,Kawamoto, Richard,Sheville, Justin,Renock, Sean,Xu, Kevin,Pokross, Matthew,Zhou, Songtao,Winter, Carol,Walter, Richard,Mekel, Marlene,Evdokimov, Artem G.
, p. 5517 - 5522 (2006)
A new series of potent 8-hydroxyquinolines was designed based on the newly resolved X-ray crystal structure of EGLN-1. Both alkyl and aryl 8-hydroxyquinoline-7-carboxyamides were good HIF-1α prolyl hydroxylase (EGLN) inhibitors. In subsequent VEGF inducti
Identification and Optimization of a Series of 8-Hydroxy Naphthyridines with Potent in Vitro Antileishmanial Activity: Initial SAR and Assessment of in Vivo Activity
Thomas, Michael G.,De Rycker, Manu,Wall, Richard J.,Spinks, Daniel,Epemolu, Ola,Manthri, Sujatha,Norval, Suzanne,Osuna-Cabello, Maria,Patterson, Stephen,Riley, Jennifer,Simeons, Frederick R. C.,Stojanovski, Laste,Thomas, John,Thompson, Stephen,Naylor, Claire,Fiandor, Jose M.,Wyatt, Paul G.,Marco, Maria,Wyllie, Susan,Read, Kevin D.,Miles, Timothy J.,Gilbert, Ian H.
supporting information, p. 9523 - 9539 (2020/10/19)
Visceral leishmaniasis (VL) is a parasitic infection that results in approximately 26 ?000-65 ?000 deaths annually. The available treatments are hampered by issues such as toxicity, variable efficacy, and unsuitable dosing options. The need for new treatments is urgent and led to a collaboration between the Drugs for Neglected Diseases initiative (DNDi), GlaxoSmithKline (GSK), and the University of Dundee. An 8-hydroxynaphthyridine was identified as a start point, and an early compound demonstrated weak efficacy in a mouse model of VL but was hampered by glucuronidation. Efforts to address this led to the development of compounds with improved in vitro profiles, but these were poorly tolerated in vivo. Investigation of the mode of action (MoA) demonstrated that activity was driven by sequestration of divalent metal cations, a mechanism which was likely to drive the poor tolerability. This highlights the importance of investigating MoA and pharmacokinetics at an early stage for phenotypically active series.
SECONDARY 8-HYDROXYQUINOLINE-7-CARBOXAMIDE DERIVATIVES FOR USE AS ANTIFUNGAL AGENTS
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Page/Page column 21, (2011/07/30)
The present invention provides secondary 8-hydroxyquinoiine-7-carboxamide derivatives of general formula (I) and pharmaceutically acceptable salts thereof. These compounds are useful as antifungal agents. Specifically, these compounds were tested against Tricophyton Rubrum, Tricophyton Mentagrophytes, Aspergillus Niger and Scopulahopsis Brevicaulis. These compounds are active against Candida species such as Candida Albicans and Candida Glabrata.
Secondary 8-hydroxyquinoline-7-carboxamide derivatives for use as antifungal agents
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Page/Page column 11, (2011/08/04)
The present invention provides secondary 8-hydroxyquinoline-7-carboxamide derivatives of general formula (I) and pharmaceutically acceptable salts thereof. These compounds are useful as antifungal agents. Specifically, these compounds were tested against Tricophyton Rubrum, Tricophyton Mentagrophytes, Aspergillus Niger and Scopulariopsis Brevicaulis. These compounds are active against Candida species such as Candida Albicans and Candida Glabrata.
8-hydroxy-7-substituted quinolines as anti-viral agents
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, (2008/06/13)
The present invention provides for 8-hydroxy-7-substituted quinoline compounds such as formula III These compounds are useful as anti-viral agents. Specifically, these compounds have anti-viral activity against the herpes virus, cytomegalovirus (CMV). Many of these compounds are also active against other herpes viruses, such as the varicella zoster virus, the Epstein-Barr virus, the herpes simplex virus and the human herpes virus type 8 (HHV-8).
