A novel ionic liquid (IL) supported, green synthetic protocol has been developed toward the synthesis of oxo and thio hydantoin analogues tethered with tetrahydro-beta-carboline by the use of focused microwave irradiation. IL-bound tryptophan underwent a Pictet-Spengler reaction with various carbonyl compounds to generate the IL-immobilized tetrahydro-beta-carbolines in aqueous isopropanol medi...

an electroorganic reaction for the synthesis of 7-amino-2, 4-dioxo-5-phenyl-2,3,4,5-tetrahydro-1h-pyrano[2, 3-d] pyrimidine-6-carbonitrile and ethyl-7-amino-2, 4-dioxo-5-phenyl-2,3,4,5-tetrahydro-1h-pyrano[2, 3-d] pyrimidine-6-carboxylate derivatives are described, using an electrogenerated base of the anion of malonitrile or ethylcyanoacetate. this one-pot, three-component condensation of an a...

New 1-phenoxymethyl-4-aryl-5,6,7,8-tetrahydro-2?,4a,8a-triazacyclopenta[ cd ]azulene-3-carboxylic (or carbothionic) acid derivatives have been designed, synthesized and evaluated for their in vitro antioxidant activity under conditions of the artificial oxidative stress using ionol, ascorbic ?-tocopherol as reference drugs. It has found that ]azulene-3-carbothionic 9b, 9c, 9d, 9e, 9f, 9i 1-phen...

Two approaches to tetrahydro-[1H]-2-benzazepin-4-ones of interest as potentially selective, muscarinic (M(3)) receptor antagonists have been developed. Base promoted addition of 2-(tert-butoxycarbonylamino)methyl-1,3-dithiane with 2-(tert-butyldimethylsiloxymethyl)benzyl chloride gave the corresponding 2,2-dialkylated 1,3-dithiane which was taken through to the dithiane derivative of the parent...

The compounds, 2-(methylsulfonyl)-1,2,3,4-tetrahydro-9H-pyrido[3,4-b]indole-3-carboxylic acid (DM3), 2-(phenylsulfonyl)-1,2,3,4-tetrahydro-9H-pyrido[3,4-b]indole-3-carboxylic acid (DM(4)), and 2-(p-toluenesulfonyl)-1,2,3,4-tetrahydro-9H-pyrido[3,4-b]indole-3-carboxylic acid (DM(5)) were synthesized by coupling of 1,2,3,4-tetrahydro-9H-pyrido[3,4-b]indole-3-carboxylic acid (DM(2)) with methanesu...

Formation of NO by NO synthases (NOSs) strictly depends on tetrahydrobiopterin. Its structural analog, tetrahydro-4-aminobiopterin, is an inhibitor of all NOS isoenzymes, which prolongs allograft survival in acute murine cardiac rejection and prevents septic shock in the rat. In this study, we show that murine bone marrow-derived dendritic cells treated with tetrahydro-4-aminobiopterin had a re...

An electroorganic reaction for the synthesis of 7-amino-2, 4-dioxo-5-phenyl-2,3,4,5-tetrahydro-1H-pyrano[2, 3-d] pyrimidine-6-carbonitrile and ethyl-7-amino-2, 4-dioxo-5-phenyl-2,3,4,5-tetrahydro-1H-pyrano[2, 3-d] pyrimidine-6-carboxylate derivatives are described, using an electrogenerated base of the anion of malonitrile or ethylcyanoacetate. This one-pot, three-component condensation of an a...

Synthesis and characterization of 6-(hydroxymethyl)-14, 16-dimethyl-13, 14, 16, 17-tetrahydro-6H-13, 17-epiminodibenzo [e, l] [1, 4] dioxacyclotridecin-15 (7H)-oneABSTRACTNew 6-(hydroxymethyl)-14, 16-dimethyl-13, 14, 16, 17-tetrahydro-6H-13, 17-epiminodibenzo [e, l] [1, 4] dioxacyclotridecin-15 (7H)-one (2a) was synthesized in good yield by the Petrenko–Kritchenko reaction of 2, 2'-((3-hydroxyp...

Compounds that interact with microtubules, such as paclitaxel, have been shown to possess protective properties against beta-amyloid (Abeta) induced neurodegeneration associated with Alzheimer's disease. In this work, the novel agent (3R,5S,7as)-(3,5-bis(4-fluorophenyl)tetrahydro-1H-oxazolo[3,4-c]oxazol-7a-yl)methanol was investigated for effectiveness in protecting neurons against several toxi...