A series of novel indole-2-carboxylate derivatives were synthesized and assayed to determine their in vitro broad-spectrum antiviral activities. The biological results showed that some of the synthesized compounds exhibited potent broad-spectrum antiviral activity. Notably, compound 8f showed the highest SI value (17.1) to Cox B3 virus. Compound 14f showed both potent inhibitory activity agains...

The chemiluminescence (CL) intensities of various indole derivatives substituted with a glyoxylyl group at the 3-position and a hydroxyl group at the 5-position of the indole ring were compared upon the addition of H2O2 in alkaline media. The CL intensities of 3-indoleglyoxylyl chloride, 3-indoleglyoxylic acid, 5-hydroxyindole and 5-benzyloxyindole in CH3CN were 5.9-, 48-, 5.9- and 3.3-fold str...

Using reversed-phase "high-performance" liquid chromatography with fluorescence detection, we separated and identified some naturally fluorescent compounds in uremic serum and hemodialysate from patients with chronic renal disease. Several of the naturally fluorescent compounds were identified as indole derivatives by co-chromatography with authentic standards. In one specific case, the identit...

Pyrazolo[4,3-b]indole derivatives have been designed as novel CK2 inhibitor compounds based on the binding mode analysis of a previously reported phenylpyrazole-type CK2 inhibitor. A series of pyrazolo[4,3-b]indoles and related dihydropyrazolo[4,3-b]indoles were efficiently prepared from simple starting materials using a gold-catalysed three-component annulation reaction as a key step. Several ...

The purely inorganic copper oxide on silica catalyzes the reaction of methyl phenyldiazoacetate with N-methyl indole under mild reaction conditions, giving the alkylation (formally a C-H insertion) in position 3, and the catalyst can be recovered and reused at least in 5 consecutive runs with only minor loss in activity. The scope of the reaction includes various diazo compounds and indole or p...

Articles you may be interested in Solvation dynamics of tryptophan in water-dimethyl sulfoxide binary mixture: In search of molecular origin of composition dependent multiple anomalies The oxidation of tyrosine and tryptophan studied by a molecular dynamics normal hydrogen electrode Molecular dynamics simulations of the rotational reorientation of tryptophan and a series of indole derivatives i...

Sepsis, a typically acute inflammatory disease, is the biggest cause of death in ICU (intensive care unit). Novel anti-inflammatory alternatives are still in urgent need. In this study, we designed and synthesized 30 indole-2-one and 7-aza-2-oxindole derivatives based on the skeleton of tenidap, and their anti-inflammatory activity was determined by evaluating the inhibitory potency against lip...

A facile and efficient synthesis of bis(indolyl)methanes derivatives (3a-u) was reported via a condensation reaction of aldehydes and indole in the presence of by silica-supported-3-(triethoxysilyl) propane-1-ammonium chloride catalysis under solvent free conditions. We studied the reaction in different conditions and optimized. The use of just 0.02 g of (silica gel-ammonium salt) is sufficient...

TFA/DMSO combination was found to efficiently promote the cross-dehydrogenative coupling of a wide range hetaryl thiols with indole derivatives, leading 3-(hetarylsulfenyl)indoles in good-to excellent yields under mild heating conditions. Two-fold hetarylsulfenylation indoles 2- and 3-positions could be conveniently achieved by simply adapting molar ratio starting materials.