- Discovery of CDK5 Inhibitors through Structure-Guided Approach
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Specific abrogation of cyclin-dependent kinase 5 (CDK5) activity has been validated as a viable approach for the development of anticancer agents. However, no selective CDK5 inhibitor has been reported to date. Herein, a structure-based in silico screenin
- Khair, Nishat Z.,Lenjisa, Jimma L.,Tadesse, Solomon,Kumarasiri, Malika,Basnet, Sunita K. C.,Mekonnen, Laychiluh B.,Li, Manjun,Diab, Sarah,Sykes, Matthew J.,Albrecht, Hugo,Milne, Robert,Wang, Shudong
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supporting information
p. 786 - 791
(2019/05/17)
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- BIARYL PYRAZOLES AS NRF2 REGULATORS
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The present invention relates to biaryl pyrazole compounds, methods of making them, pharmaceutical compositions containing them and their use as NRF2 regulators.
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Page/Page column 285; 286
(2017/08/01)
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- Discovery, synthesis, and structure-activity relationships of 2-aminoquinazoline derivatives as a novel class of metabotropic glutamate receptor 5 negative allosteric modulators
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A virtual screening approach using various in silico methodologies led to the discovery of 2-(m-tolylamino)-7,8-dihydroquinazolin-5(6H)-one (1) as a moderately active negative allosteric modulator (NAM) of the metabotropic glutamate receptor subtype 5 (mGluR5) showing high selectivity against the subtype mGluR1. Modifications of the parent compound by rational design yielded a series of highly potent derivatives which will serve as valuable starting points for further hit-to-lead optimization efforts toward a suitable drug candidate for the treatment of l-DOPA induced dyskinesia.
- Kubas, Holger,Meyer, Udo,Krueger, Bjoern,Hechenberger, Mirko,Vanejevs, Maksims,Zemribo, Ronalds,Kauss, Valerjans,Ambartsumova, Raisa,Pyatkin, Ilya,Polosukhin, Alexey I.,Abel, Ulrich
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supporting information
p. 4493 - 4500
(2013/08/23)
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- METABOTROPIC GLUTAMATE RECEPTOR MODULATORS
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The invention relates to heterocyclic derivatives as well as their pharmaceutically acceptable salts. The invention further relates to a process for the preparation of such compounds. The compounds of the invention are mGluR5 modulators and are therefore useful for the control and prevention of acute and/or chronic neurological disorder
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Page/Page column 50-51
(2012/07/13)
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- Synthesis of δ-tributylstannyl-α,βγ, δ-unsaturated aldehydes from pyridines
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(Equation Presented) Zincke aldehydes, which are readily available from the ring-opening reaction of pyridinium salts, are easily converted into δ-tributylstannyl-α,β,γ,δ-unsaturated aldehydes (stannyldienals) by the action of tributylstannyllithium. This reaction appears to proceed via 1,6-stannyllithium addition/elimination of lithium dialkylamide. Several stannyldienals of significant utility for the synthesis of polyene natural products have been made by this route, which proceeds in modest yields, but is successful on multigram scale using inexpensive reagents. Simple stannylenals and stannylenones are similarly available from the corresponding vinylogous amides.
- Michels, Theo D.,Rhee, Jong Uk,Vanderwal, Christopher D.
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body text
p. 4787 - 4790
(2009/05/07)
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- Tricyclic 6-alkylidene-penems as class-D beta-lactamases inhibitors
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This invention relates to certain tricyclic 6-alkylidene penems which act as a inhibitor of class-D enzymes. β-Lactamases hydrolyze β-lactam antibiotics, and as such serve as the primary cause of bacterial resistance. The compounds of the present inventio
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Page/Page column 26
(2010/11/25)
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- THE SYNTHESIS OF MANNICH BASES FROM KETONES AND ESTERS VIA ENAMINONES.
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The reactions of a series of activated methylene compounds with amide acetals to form high yields of enaminones is described.Further conversion to the Mannich bases via reduction with lithium aluminium hydride is also covered.
- Schuda, Francis Paul,Ebner, Cynthia B.,Morgan, Tina M.
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p. 2567 - 2570
(2007/10/02)
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