The article provides the first example of metal-catalyzed aryl disulfide addition to unsubstituted acetylene. The use of inexpensive Ni(acac)2 precatalyst with phosphine ligands results in competitive formation of (Z)-1,2-bis(arylthio)ethenes and (Z,Z)-1,4-bis(arylthio)buta-1,3-dienes. The proce...

The synthesis, characterization, crystal structure and computational studies of a new tetranuclear Cu(I)–triazene cluster complex is reported. The tetranuclear cluster complex, Cu4L4, is obtained by the reaction of 1,3-bis(4-bromophenyl)triazene (HL) and [Cu(CH3CN)4]PF6 in THF solvent in the pr...

This review presents a systematic and comprehensive survey of the utility of 4-hydroxy-2(1H)-quinolone as a building block of heterocyclic compounds. The reaction mechanism is considered as well as the scope and limitation of the most important of these approaches are demonstrated.

The syntheses of 2,3-dihydro-4-quinolones from 2-propargylphenylcarbamates by one-pot tandem process that involves Meyer-Schuster rearrangement or arylative Meyer-Schuster rearrangement/Michael addition of carbamate nitrogen to the resulting vinyl ketones have been developed. Phenylcarbamates te...

The 4-quinolones and their analogs are a heterogeneous group of biologically active compounds that have evolved in modern days to provide utilities at the forefront of antibiotic research. They have been used to combat Gram-negative or Gram-positive bacteria, suppress tumor growth, and treat man...

The intracellular distribution of radioactivity in mammary tumors has been studied following administration of tritiated podophyllic acid ethyl hydrazide to tumorbearing R III mice. Over 90 per cent of the label is found in the 100,000 g supernatant, two thirds of which is associated with two pr...

Administration of podophyllic acid ethyl hydrazide to mice bearing spontaneous mammary tumors, suppresses the incorporation of radioactive precursors into the nucleic acids of the neoplastic tissue. This suppression was also observed in the case of liver nucleic acids but with exceptions in a nu...

This work optimized the novel biotransformation process of podophyllotoxin to produce podophyllic acid by Pseudomonas aeruginosa CCTCC AB93066. Firstly, the biotransformation process was significantly affected by medium composition. 5 g/l of yeast extract and 5 g/l of peptone were favorable for ...

Epitetrodotoxin (6-epiTTX) and 11-deoxytetrodotoxin (11-deoxyTTX), isolated from an Okinawan newt, Cynops ensicauda, were tested for sodium-channel blocking effects on the voltage-clamped frog skeletal muscle fiber. In 6-epiTTX, the C-6 -OH is in an epimeric position; in 11-deoxyTTX, C-11 has a ...

Tetrodotoxin was detected in all nine species of newts tested, 6-epitetrodotoxin in six species, and 11-deoxytetrodotoxin in five species. Only one species lacked the analogues, thus suggesting that the analogues were common metabolites among newts. Toxin levels were high in Taricha granulosa an...

The purpose of this study was to synthesize the library of 33 new N-benzyl-2-(2,5-dioxopyrrolidin-1-yl)propanamides, 2-(3-methyl-2,5-dioxopyrrolidin-1-yl)propanamides, and 2-(2,5-dioxopyrrolidin-1-yl)butanamides as potential new hybrid anticonvulsant agents. These hybrid molecules join the chemi...

By using functionality inversion approach, we identified a new scaffold containing (S)-α-phenyl-γ-amino butanamide as CCR5 antagonists derived from the 1,3-propanediamine carboxamide pharmacophore protocol. The (2S)-2-phenyl-4-(8-aza-bicyclo[3.2.1]octan-8-yl)-butanamide derivatives display sig...

We identified novel potent inhibitors of p38 MAP kinase using structure-based design strategy. X-ray crystallography showed that when p38 MAP kinase is complexed with TAK-715 (1) in a co-crystal structure, Phe169 adopts two conformations, where one interacts with 1 and the other shows no interac...

This article describes the chemical synthesis, ADME and pharmacological properties and early safety pharmacology evaluation of a series of novel Nurr1/NOT agonist. It is meant as a support to an article recently published in Bioorganic and Medicinal chemistry Letters and entitled “Development o...

An inversion of electro-mechanical coupling: namely, mechanical relaxation which precedes electrical repolarization, has been proposed as a surrogate marker to predict the occurrence of drug-induced arrhythmias. The present study was designed to qualitatively and quantitatively clarify the effec...

We analyzed torsadogenic and pharmacokinetic profile of E-4031 using chronic atrioventricular block dogs. E-4031 in intravenous doses of 0.03, 0.1 and 0.3 mg/kg over 10 min prolonged QT/QTc, and increased short-term variability of QT in a dose-related manner (n = 4), resulting in onset of torsad...

Baohuoside I (also known as Icariside II) is a flavonoid isolated from Epimedium koreanum Nakai. Although Baohuoside I exhibits anti-inflammatory and anti-cancer activities, its molecular targets/pathways in human lung cancer cells are poorly understood. Therefore, in the present study, we inves...

A rapid and efficient baohuoside I preparation method was established. A uniform design coupled with subset selection was employed to determine pH, reaction time, and temperature parameters, as well as dextranase hydrolysis efficiency. Hydrolysis parameters were optimized using response surface ...

Baohuoside I has better in vivo bioactivities than Icariin. Its preparation methods, such as acid hydrolysis, are of low efficiency, with undesirable byproducts. The objective of this study was to establish a novel catalysis system for its clean and efficient preparation via biphase enzymatic hy...

The aim of the present study was to investigate the anti-osteoporotic activity of Baohuoside I, an active component of Herba Epimedii. Effects of Baohuoside I on the differentiation of BMSCs and the formation of adipocytes were evaluated using alkaline phosphatase staining and methylene blue sta...