Novel selective thiadiazine DYRK1A inhibitor lead scaffold with human pancreatic β-cell proliferation activity.
Sign Up to like & getrecommendations! Published in 2018 at "European journal of medicinal chemistry"
DOI: 10.1016/j.ejmech.2018.08.007
Abstract: The Dual-Specificity Tyrosine Phosphorylation-Regulated Kinase 1A (DYRK1A) is an enzyme that has been implicated as an important drug target in various therapeutic areas, including neurological disorders (Down syndrome, Alzheimer's disease), oncology, and diabetes (pancreatic β-cell… read more here.
Keywords: dyrk1a; pancreatic cell; dyrk1a inhibitor; thiadiazine ... See more keywords
Two-step conversion of 3,4,4,5-tetrachloro-4H-1,2,6-thiadiazine into 4,5,6-trichloropyrimidine-2-carbonitrile
Sign Up to like & getrecommendations! Published in 2017 at "Tetrahedron Letters"
DOI: 10.1016/j.tetlet.2017.05.082
Abstract: Abstract Tin reduction of 3,4,4,5-tetrachloro-4 H -1,2,6-thiadiazine afforded perchloro-9-thia-1,5,8,10-tetraazaspiro[5.5]undeca-1,4,7,10-tetraene (10%) and 3,5-dichloro-4 H -1,2,6-thiadiazine-4-thione (27%), the structures of which were supported by single crystal X-ray crystallography. Treating the tetrachlorothiadiazine with Ph 3 P (1 equiv.) afforded… read more here.
Keywords: trichloropyrimidine carbonitrile; tetrachloro thiadiazine; two step; thiadiazine ... See more keywords
Reaction of 3,4,4,5-tetrachloro-4H-1,2,6-thiadiazine with benzyltriethylammonium chloride
Sign Up to like & getrecommendations! Published in 2018 at "Tetrahedron Letters"
DOI: 10.1016/j.tetlet.2018.08.007
Abstract: Abstract 3,4,4,5-Tetrachloro-4H-1,2,6-thiadiazine was reacted with BnEt3NCl (10 mol%) to give perchloro-9-thia-1,5,8,10-tetraazaspiro[5.5]undeca-1,4,7,10-tetraene (up to 18% yield), 4,5,6-trichloropyrimidine-2-carbonitrile (up to 44% yield) and four minor side products: 2,7-dichlorothiazolo[5,4-d]pyrimidine-5-carbonitrile, 2-(4-chloro-6H-thiazolo[5,4-c][1,2,6]thia-diazin-6-ylidene)malononitrile, 4,8-dichloropyrrolo[2′,1′:2,3]imidazo[4,5-c][1,2,6]thiadiazine-6,7-dicarbonitrile and 4,7-dichloro-[1,2,6]thiadiazino[3,4-b]thiazolo[5,4-e][1,4]diazepin-9(10H)-one. Single crystal X-ray studies support the… read more here.
Keywords: benzyltriethylammonium chloride; thiadiazine benzyltriethylammonium; reaction tetrachloro; thiadiazine ... See more keywords