209204-23-9Relevant academic research and scientific papers
SIDEROPHORE CONJUGATED PYRAZOLIDINONES, AND ANALOGUES THEREOF
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Page/Page column 29, (2020/02/14)
In one aspect, the invention provides compounds and methods that are useful for treating bacterial infections.
Pharmacological validation of trypanosoma brucei phosphodiesterases B1 and B2 as druggable targets for African sleeping sickness
Bland, Nicholas D.,Wang, Cuihua,Tallman, Craig,Gustafson, Alden E.,Wang, Zhouxi,Ashton, Trent D.,Ochiana, Stefan O.,McAllister, Gregory,Cotter, Kristina,Fang, Anna P.,Gechijian, Lara,Garceau, Norman,Gangurde, Rajiv,Ortenberg, Ron,Ondrechen, Mary Jo,Campbell, Robert K.,Pollastri, Michael P.
experimental part, p. 8188 - 8194 (2012/01/13)
Neglected tropical disease drug discovery requires application of pragmatic and efficient methods for development of new therapeutic agents. In this report, we describe our target repurposing efforts for the essential phosphodiesterase (PDE) enzymes TbrPDEB1 and TbrPDEB2 of Trypanosoma brucei, the causative agent for human African trypanosomiasis (HAT). We describe protein expression and purification, assay development, and benchmark screening of a collection of 20 established human PDE inhibitors. We disclose that the human PDE4 inhibitor piclamilast, and some of its analogues, show modest inhibition of TbrPDEB1 and B2 and quickly kill the bloodstream form of the subspecies T. brucei brucei. We also report the development of a homology model of TbrPDEB1 that is useful for understanding the compound-enzyme interactions and for comparing the parasitic and human enzymes. Our profiling and early medicinal chemistry results strongly suggest that human PDE4 chemotypes represent a better starting point for optimization of TbrPDEB inhibitors than those that target any other human PDEs.
Palladium-catalyzed annulation of haloanilines and halobenzamides using norbornadiene as an acetylene synthon: A route to functionalized indolines, isoquinolinones, and indoles
Thansandote, Praew,Hulcoop, David G.,Langer, Michael,Lautens, Mark
supporting information; experimental part, p. 1673 - 1678 (2009/07/17)
A general procedure for the palladium-catalyzed annulation of substituted haloanilines with norbornadiene gives functionalized indolines in 51-98% yield. These indolines can be rapidly converted to benzenoid- substituted indoles and tricyclic indolines. Extension to the use of substituted halobenzamides gives functionalized isoquinolinones in up to 86% yield.
