Novel N-amino benzylthiolates were synthesized via multicomponent reaction of malononitrile, isothiocyanates and benzyl halides under conventional and solvent-free conditions. Various electron-donating and -withdrawing substitutes within both isothiocyanates and benzyl halides were used to demonstrate the efficiency of new methodology. A broad spectrum of antibacterial and antifungal activities...

We have already shown that the in-vacuum gas-phase Meerwein reaction of (thio)acylium ions is general in nature and useful for class-selective screening of cyclic (thio)epoxides. Herein we report that this gas-phase reaction can also be performed efficiently at atmospheric pressure under both electrospray ionization (ESI) and atmospheric pressure chemical ionization (APCI) conditions. This alte...

β-carboline consists of a pyridine ring fused to an indole skeleton; it possesses numerous pharmacological activities, including anticancer. Previously, we reported satisfactory 2D and 3D QSAR study on derivatives. Based studies, designed, synthesized, characterized, screened fourteen derivatives for anticancer activity. Eleven them demonstrated potent activity against both liver (HepG2) adenoc...

A new click chemistry generated artificial metallonuclease is reported in the Research Article by Andrew Kellett et al. (e202305759). The oxidative DNA damaging properties of a polynuclear copper binding ligand called TC-Thio demonstrated. Copper-TC-Thio binds minor groove genomic and promotes damage via superoxide linked mechanism. inset picture shows ions, bound to ligand, melting into duplex...

The antibacterial activity of 2-thiouracil, 2-methylthiouracil, 2-hydrazinouracil, 2,4-dithiouracil, 2-thio-4-hydrazinouracil, 2-thio-6-azathymine, 2-hydrazino-6-azathymine, 2,4-dithio-6-azathymine, 2-thio-4-hydrazino-6-azathymine, 2,4-dimethylthio-6-azathymine, 2-methylthio-4-hydrazino-6-azathymine, 4-thio-6-azauracil and 4-hydrazino-6-azauracil has been studied on the growth o f : Staphylococ...

in this work, benzyl alcohol was obtained in 96% excellent yield by hydrolysis of benzyl chloride catalyzedby the recyclable temperature-dependant phase-separation system that comprised the ionic liquid peg1000-dail[bf4], toluene and ferric sulfate under homogeneous catalysis in aqueous media. this novel methodnot only enhanced the yield, but also made the operating units easy workup. the catal...

Whole-cell patch-clamp was used to assess the modulatory effect of thiopental (Thio) on glycine (Gly) receptor in mechanically dissociated rat spinal dorsal horn neurons. It was found that Thio inhibited the amplitude, accelerated the desensitization and prolonged the deactivation of Gly-induced currents (IGly) in a concentration-dependent manner. In addition, a rebound current occurred after w...

Previous studies have shown that the phenylisothiocyanate tropane analog 2-beta-propanoyl-3-beta-(2-naphthyl)-8-[4-isothiocyanato)benzyl]nortropane (HD-205) binds covalently to dopamine and serotonin transporters (DAT and SERT, respectively) in rat brain membranes (Biochem Pharmacol 74:336-344, 2007). The present study evaluated the irreversible effects of HD-205 in vivo in rats after intracran...