A catch-and-release strategy for the combinatorial synthesis of 4-acylamino-1,3-thiazoles as potential CDK5 inhibitors

Two-dimensional libraries of 4-acylamino-1,3-thiazoles 9 were prepared via Curtius rearrangement of 1,3-thiazole-4-carbonyl azides 6, trapping of the intermediate isocyanates with oxime resin, and thermal regeneration of the isocyanates from the washed resin in the presence of nucleophiles. Several...

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Veröffentlicht in:	Bioorganic & medicinal chemistry letters 2003-10, Vol.13 (20), p.3491-3495
Hauptverfasser:	LARSEN, Scott D, STACHEW, Carl F, CLARE, Paula M, CUBBAGE, Jerry W, LEACH, Karen L
Format:	Artikel
Sprache:	eng
Schlagworte:	Biological and medical sciences Combinatorial Chemistry Techniques Cyclin-Dependent Kinase 5 Cyclin-Dependent Kinases - antagonists & inhibitors Enzyme Inhibitors - chemical synthesis Enzyme Inhibitors - pharmacology Medical sciences Neuropharmacology Pharmacology. Drug treatments Psychoanaleptics: cns stimulant, antidepressant agent, nootropic agent, mood stabilizer..., (alzheimer disease) Psychology. Psychoanalysis. Psychiatry Psychopharmacology Thiazoles - chemical synthesis Thiazoles - pharmacology
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