1207754-99-1Relevant articles and documents
ALKYNYL QUINAZOLINE COMPOUNDS
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, (2021/02/19)
The present disclosure relates to compounds of Formula (I'): and pharmaceutically acceptable salts and stereoisomers thereof. The present disclosure also relates to methods of preparation these compounds, compositions comprising these compounds, and methods of using them in the prevention or treatment of abnormal cell growth in mammals, especially humans.
Synthesis and biological evaluation of antifungal derivatives of enfumafungin as orally bioavailable inhibitors of β-1,3-glucan synthase
Heasley, Brian H.,Pacofsky, Gregory J.,Mamai, Ahmed,Liu, Hao,Nelson, Kingsley,Coti, Ghjuvanni,Peel, Michael R.,Balkovec, James M.,Greenlee, Mark L.,Liberator, Paul,Meng, Dongfang,Parker, Dann L.,Wilkening, Robert R.,Apgar, James M.,Racine, F.,Hsu, Ming Jo,Giacobbe, Robert A.,Kahn, Jennifer Nielsen
, p. 6811 - 6816,6 (2020/09/02)
Orally bioavailable inhibitors of β-(1,3)-d-glucan synthase have been pursued as new, broad-spectrum fungicidal therapies suitable for treatment in immunocompromised patients. Toward this end, a collaborative medicinal chemistry program was established based on semisynthetic derivatization of the triterpenoid glycoside natural product enfumafungin in order to optimize in vivo antifungal activity and oral absorption properties. In the course of these studies, it was hypothesized that the pharmacokinetic properties of the semisynthetic enfumafungin analog 3 could be improved by tethering the alkyl groups proximal to the basic nitrogen of the C3-aminoether side chain into an azacyclic system, so as to preclude oxidative N-demethylation. The results of this research effort are disclosed herein.
ANTIFUNGAL AGENTS
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Page/Page column 54-55, (2010/04/03)
Novel derivatives of enfumafungin are disclosed herein, along with' their pharmaceutically acceptable salts, hydrates and prodrugs. Also disclosed are compositions comprising such compounds, methods of preparing such compounds and method of using such compounds as antifungal agents and/or inhibitors of (l,3)-β-D-glucan synthase. The disclosed compounds, their pharmaceutically acceptable salts, hydrates and prodrugs, as well as compositions comprising such compounds, salts, hydrates and prodrugs, are useful for treating and/or preventing fungal infections and associated diseases and conditions.