In Vitro and In Vivo Effects of R023–6152 on Heart Mitochondrial Calcium and Energy Metabolism

Remarkable Synthesis of 2-(Z)-6-(E)-4H-[1,4]-Thiazepin-5-ones by Zwitterionic Rhodium-Catalyzed Chemo- and Regioselective Cyclohydrocarbonylative Ring Expansion of Acetylenic Thiazoles

“…Thiazepinones are pharmacologically important compounds for the treatment of cancer, heart, and inflammatory diseases. These heterocycles aid in treating disease by acting as inhibitors to angitensin converting enzyme (ACE), neutral endopeptidase (NEP), leukocyte adherence, and the inhibition of calcium release in heart mitochondria . These seven-membered heterocycles have been prepared by incorporating addition, condensation, coupling, rearrangement, and thermolysis 8 methodologies in multistep syntheses.…”

Synthesis of Thiazine and Thiazepine Derivatives from (Z)-2-Cyano-3-Mercapto-3-(Phenylamino)Acrylamide

“…Method B: Reaction of 1 with 2,3-dichloro-1,4-naphthoquinone (10): Equimolar amounts of 1 and 2.3-dichloro-1,4-naphthoquinone (10) in absolute ethanol was heated under reflux conditions for 2-3 h. A yellow precipitate was formed, the formed precipitate was collected, washed by hot ethanol and recrystallised by DMF/EtOH to give the previous product 9. 4,6,5,6,4] Reaction of 1 with 2-dicyanomethyleneindan-1,3-dione (13): Mixing equimolar amounts of 1 and 13 dissolved in dry ethyl acetate. A charge transfer complex was formed (bluish-green colour).…”

“…[1][2][3] Several derivatives of 1,4-thiazepin-5-one and 2,4-dione are being developed for the treatment of cancer and heart diseases. [4][5][6] Mercaptoacrylamide derivatives are used in the syntheses of functionalised heterocyclic systems including pyrimidines, 1,3-thiazines, pyridines, pyrazoles, thiazoles, isothiazoles, and thiophenes. [7][8][9][10][11][12] Based on the condensation of 3-alkylthio-2-cyano-3-mercaptoacrylamide with carbonyl compounds (aldehydes and ketones) under acidic conditions, Yokoyama found a convenient synthetic route to 2,5,6substituted 2,3-dihydro-1,3-thiazin-4(1H)-ones.…”