The mechanism of N-acetyl-p-benzoquinone imine (NAPQI)-induced release of Ca2+ from rat liver mitochondria was investigated. The addition of NAPQI or 3,5-Me2-NAPQI (a dimethylated analogue of NAPQI with only oxidizing properties) to mitochondria resulted in the rapid and extensive oxidation of NADH and NADPH. High-performance liquid chromatographic analysis of mitochondrial pyridine nucleotides...

Vabicaserin is a potent 5-hydroxytryptamine(2C) agonist that is currently being developed for the treatment of the psychotic symptoms of schizophrenia. In this study, in vitro and in vivo metabolism of vabicaserin was evaluated in mice, rats, dogs, monkeys, and humans, and the structures of the metabolites were characterized by liquid chromatography/mass spectrometry and NMR spectroscopy. Vabic...

Direct evidence of complex prebiotic chemistry from a water-rich world in the outer solar system is provided by the 4.5-billion-year-old halite crystals hosted in the Zag and Monahans (1998) meteorites. This study offers the first comprehensive organic analysis of the soluble and insoluble organic compounds found in the millimeter-sized halite crystals containing brine inclusions and sheds ligh...

When the reagents LAlMe (L = N,N'-(alkylene or arylene)bis(3,5-di-tert-butyl)salicylideneimine (alkylene = ethylene (Salen(tBu))(1), propylene (Salpen(tBu))(2), and butylene (Salben(tBu)) (3); arylene = phenylene (Salophen(tBu) (4), 3,4-dimethylphenylene (Salomphen(tBu) (5)) are combined with Ph(H)P(O)OH in tetrahydrofuran (thf) the unique aluminophosphinate compounds, [L(tBu)Al[O(2)P(H)Ph]](n)...

A series of new 5-imino-4-thioxo-2-imidazolidinone derivatives 3 with various halogenated and alkylated aromatic substituents at N1 and N3 was synthesized. Imidazolidineiminothione derivatives 3 were prepared from the reaction of N-arylcyanothioformamide derivatives with aryl isocyanates. These compounds were used as key synthons for the preparation of wide variety of new substituted imidazole ...

Fungal infections threaten human health, particularly in immune-compromised patients worldwide. Although there are a large number of antifungal agents available, the desired clinical attributes for the treatment of fungal infections have not yet been achieved. Azoles are the mainstay class of the clinically used antifungal agents. In the current study, the synthesis, spectroscopic characterizat...

ARIOUS alkylating agents have long been used for inducing mutations and Vchromosome breaks in some plants and animals. Effects on Drosophila spermatogenesis have been investigated by AUERBACH (1940, 1949, 1958), especially with mustard gas, and FAHMY and FAHMY (1953, 1956) used various compounds. All types of mutations have so far been obtained-dominant lethals and semilethals, recessive lethal...

A convenient synthesis of novel bi/tricyclic azasugars fused thiazolidin-4-one and thiazinan-4-one by the one-pot tandem Staudinger/aza-Wittig/cyclization reaction under microwave radiation was demonstrated. The reactions were carried out with the azidosugar 1 and mercaptan acids via a key intermediate Schiff base and stereoselectively afforded the titled bi/tricyclic azasugars in good yield. A...

Methods for imine trifluoromethylation are of great importance because amines with trifluoromethylated stereogenic centers are useful building blocks for synthetic chemistry and drug discovery. Herein, we describe a new copper(II)-catalyzed imine trifluoromethylation method without the use of Lewis base activators, presumably through cooperative activation.