An efficient method for the synthesis of polyfunctional imidazoles from vinyl azides and amidine has been developed. Starting from vinyl azide and amidine, this transformation proceeds without any additives and the obtained imidazoles can be decorated with ester functional group that is a promis...

We investigated twelve benzyl phenyl ketone derivatives which are synthetic precursors of isoflavonoids that are shown be good 5-hLOX inhibitors, especially those that have the catechol group, but these precursors never have been assayed as 5-hLOX inhibitors being a novelty as inhibitors of the ...

AXM, when subcutaneously injected during the first 3 min following the acquisition of a nondiscriminative instrumental learning task, induced an aversion for the food reinforcement which had been associated with the training situation and with the pharmacological treatment. The high number of no...

Cycloheximide (CHX) is an inhibitor of protein synthesis and commonly used to modulate death receptor-mediated apoptosis or to induce apoptosis in a number of normal and transformed cells. In this study we show that a close structural derivative of CHX, acetoxycycloheximide (E-73) induced rapid ...

Acetoxycycloheximide (ACH), the most potent inhibitor of protein synthesis in mammalian tissues, was administered to female rats in order to investigate the relationship of hepatic protein synthesis inhibition to the pathogenesis of fatty liver. Groups of animals were sacrificed at intervals bet...

The intraperitoneal administration of acetoxycycloheximide to rats in vivo stimulates the incorporation of l-(14C)-phenylalanine into protein in a liver microsomal system in vitro after 24 hours. The increased incorporation of the system is associated predominantly with the microsomal fraction a...

The effects of acetoxycycloheximide (AXM) (7 mg/kg) and anisomycin (ANI) (25 and 150 mg/kg) on approach and escape responses induced by hypothalamic stimulation were studied in a situation in which male Swiss mice could initiate a continuous brain stimulation train by pressing a lever at one end...

Tumor necrosis factor (TNF)-α activates the nuclear factor κB (NF-κB) signaling pathway. The protein synthesis inhibitor cycloheximide (CHX) and its structural derivative acetoxycycloheximide (Ac-CHX) have been recently shown to block the TNF-α-induced activation of NF-κB via ectodomain she...

Benzylation of phenol was successfully achieved in water under room temperature mediated by tetrabutylammonium bromide (TBAB) for only 2 h affording the corresponding benzyl phenyl ether with good to excellent yields. This protocol is very efficient, simple, avoiding catalysts, easy to work-up a...

A novel series of melatonin-derived benzylpyridinium bromides have been designed, synthesized, and evaluated as multi-functional anti-AD agents with cholinesterase inhibitory, antioxidant, and neuroprotective activities. In vitro studies showed that most of these compounds exhibited potent inhib...

The nucleophilic trifluoromethylthiolation of benzyl bromides using (bpy)Cu(SCF3) gave the desired products of benzyl trifluoromethyl sulfides in good to excellent yields. A diverse set of important functional groups including cyano, nitro, ester, alkoxy, halide, and heterocyclic groups can be w...

We previously reported that 4-(pyrrolidin-1-yl)benzonitrile derivative 1b was a selective androgen receptor modulator (SARM) that exhibited anabolic effects on organs such as muscles and the central nervous system (CNS), but neutral effects on the prostate. From further modification, we identifi...

Nerve growth factor receptor (NGFR), a member of kinase protein, is emerging as an important target for Glioblastoma (GBM) treatment. Overexpression of NGFR is observed in many metastatic cancers including GBM, promoting tumor migration and invasion. Hydrazones have been reported to effectively ...

The second-order rate constants for the nucleophilic replacement of fluorine by isopropoxide in 5,6,7,8-tetrafluoro- and 6,7,-difluoro-1,2,3,4-tetrahydro-9-alkenyl-1,4-methanonaphthalenes and related 9-alkyl systems have been measured. A factor of 6 - 7 separates the most reactive compounds [the...

Vinyl acetate is used as an acetylene equivalent in rhodium(III)-catalysed C-H activation/annulation with aryl ketoxime esters. Extension to an aldoxime ester allows for a concise formal synthesis of decumbenine B.

The present study examined the electronic dynamics of 4,5-dimethoxy-2-nitrobenzyl acetate after π-π* excitation. Pump-probe measurement using a near-ultraviolet sub-10 fs pulse laser revealed that the lifetime of the S*(π-π*) state is 500 fs after photoexcitation to produce the S*(n-π*) sta...

Erythrocyte acetylcholinesterase (AChE) is a preferred biomarker for the detection of organophosphorus poisoning. Acetylthiocholine (ATCh) is the most popular substrate for the detection of AChE activity. However, oximolysis is a prominent feature with ATCh. In this context, we have searched alt...

Methylation of histone arginine residues is an epigenetic mark related to gene expression that is implicated in a variety of biological processes and can be reversed by small-molecule modulators of protein arginine methyltransferases (PRMTs). A series of symmetrical ureas, designed as analogues ...

3-Naphthoyl- and 3-phenylacetylindoles represent a group of substances of cannabimimetic activity with affinities – strongly influenced by their functional groups – to cannabinoid receptors CB1 and CB2. Some of them have been described as ingredients of herbal blends also known as “smart prod...

A method is described for the synthesis, purification and radiolabelling of [123I/131I]2-{5-(4-iodophenyl)-pentyl}oxirane-2-carboxylic acid ethyl ester. For the synthesis of this new agent, 5-phenylpentyl bromide (1), synthesized by reacting 5-phenyl-I-pentanol with sodium bromide under acidic c...