1-[6-[[17β-3-Methoxyestra-1,3,5(10)-trien-17-yl]amino]-hexyl]1H-pyrrole-2,5-dione (U-73122) is an aminosteroid that was identified initially as a potent inhibitor of platelet activation by receptor-specific agonists. U-73122 inhibits receptor-coupled generation of inositol 1,4,5-trisphosphate (...

We studied the effects of the aminosteroid U-73122, a putative phospholipase C (PLC) inhibitor, on carbachol-induced increases in insulin release, [Ca2+]i, and IP3 in β-TC3 cells. Carbachol (0.1–100 μM) increased [Ca2+]i and carbachol (0.1–1000 μM) increased insulin release dose-dependently...

We propose a simple strategy that combines polymerization with chemical activation to prepare a new high-surface-area nitrogen-doped porous carbon (SU-NPC) using sucrose as a carbon precursor, urea as a nitrogen precursor and KOH as an activation reagent. Additionally, this method avoids the tim...

The production of n-butanol from sugarcane juice by metabolically engineered Clostridium tyrobutyricum Ct(Δack)-pscrBAK overexpressing scr operon genes (scrB, scrA, and scrK) for sucrose catabolism and an aldehyde/alcohol dehydrogenase gene (adhE2) for butanol biosynthesis was studied with corn...

To explore the effect of fluorine atom on photophysical properties, in this work, we synthesized three new small molecules (SMs) with acceptor-donor-acceptor (A-D-A) configuration, SM-0F, SM-2F and SM-4F, where 4,8-bis(octyloxy)benzo[1,2-b:4,5-b']dithiophene (BDT) as the electron-donating a...

It has been found that modified benzotriazoles: (2-(2-hydroxy-3-chlormethylacetamid-5-methylphenyl)2H-benzotriazole, 2-(2-hydroxy-3[(N,N-di-n-butyl)acetamidmethyl]-5-methyl-phenyl)2H-benzotriazole and 2-(2-hydroxy-3[(N,N-di-n-octyl)acetamidmethyl]-5-methyl-phenyl)2H-benzotriazole) have photostab...

Substituted diphenylamine antioxidants (SDPAs) and benzotriazole UV stabilizers (BZT-UVs) are contaminants of emerging environmental concern. However, little is known about the occurrence of these contaminants in the Arctic. In this study, we investigated the levels of 11 SDPAs and 6 BZT-UVs in ...

Women, most of whom had regular menstrual cycles, were administered [d-Leu6,des-Gly10-NH2]-luteinizing hormone-releasing hormone (LH-RH) ethylamide (d-Leu6-LH-RH-EA) via different routes during the early or midfollicular phase of the cycle. Plasma LH, follicle-stimulating hormone (FSH), and estr...

The synthesis of 6-iodo-4-trifluoromethylisatin, an intermediate in the synthesis of the growth hormone secretagogue SM-130686, is disclosed. The synthesis is achieved in seven steps, with an overall yield of 32%, and requires a single recrystallisation as the only purification step. 2-Methyl-3-...

Trifluoromethylated enynyl sulfones 3 were reacted with PhLi at −78 °C for 2–4 h to give 2-trifluoromethyl-1,1-diphenyl-1,3-enynes 6 in good yields. Carbocyclization reaction of 6 with 10 mol% of Pd(OAc)2 in cosolvent of CF3COOH and MC (4:1) at room temperature for 1 h afforded 2-trifluorometh...

Monochiral α-benzamidocinnamic esters of N-methylephedrine or mandelic derivatives and benzylidene or alkylidene diketopiperazines, all obtained from oxazolones, react with diazomethane to give moderate to high diastereomeric excesses (d.e.) of pyrazoline derivatives which, after photolysis and...

The stereoselective synthesis of (1R,2R)- and (1S,2S)-trans-2-(diphenylmethylideneamino)cyclopropanecarboxylic acid has been accomplished in six steps starting from (2S)- and (2R)-β-benzyl N-(tert-butoxycarbonyl)aspartate, respectively. The key-step in the reaction sequence is a stereoselective...

Wohlfahrtia magnifica is the main agent of traumatic myiasis in the southern Palaearctic zone. It was recorded in outbreak situations in Crete, Greece, for the first time in 1999, causing widespread production losses and considerable concern in the livestock sectors. Most commonly applied curati...

MTB lysine-ɛ-aminotransferase (LAT) was found to play a crucial role in persistence and antibiotic tolerance. LAT serves as a potential target in the management of latent tuberculosis. In present work we attempted to derivatize the benzothiazole lead identified through high throughput virtual sc...

Based on the structure of HIV-1 gp41 binding site for small-molecule inhibitors, optimization of lead 2 resulted in the discovery of a new series of 2,5-dimethyl-3-(5-(N-phenylrhodaninyl)methylene)-N-(3-(1H-tetrazol-5-yl)phenyl)pyrrole compounds with improved anti-HIV-1 activity. The most active...

RésuméThe synthesis of N-(1H-tetrazol-5-yl) azetidin-2-one and the racemic 4-methyl and 4-trifluoromethyl analogues starting with 5-amino tetrazole via two Independent pathways is described. The compounds were devoid of any useful antibacterial activity.

Monoamine transporters regulate the concentration of monoamine neurotransmitters, which are essential for vital physiological processes, and their dysfunction can cause several central nervous system diseases. Monoamine transporters currently appear to be the potential target in the management o...

A novel hydrazone derivative 2-bromo-4-chloro-6-{[4-(3-methyl-3-phenyl-cyclobutyl)-thiazol-2-yl]-hydrazonomethyl}-phenol was synthesized and characterized by IR, UV–Vis spectroscopy and X-ray single crystal diffraction. The compound crystallizes in monoclinic space group P21/c with a = 8.0862(3...

The thiaminalisation of 2-amino-2-(mercaptomethyl)propane-1,3-diol [‘2-(hydroxymethyl)cysteinol’] with aryl(di)aldehydes is reported. The resulting new class of 2-aryl-4,4-bis(hydroxymethyl)-1,3-thiazolidines is investigated by NMR and IR spectroscopy in tandem with DFT calculations, permittin...

The conformationally restricted S-adenosylmethionine analogue AdoMac (S-(5′-deoxy-5′-adenosyl)-1-ammonio-4-methylsulfonio-2-cyclopentene has been shown to act as an enzyme activated, irreversible inhibitor of the Escherichia coli form of the enzyme S-adenosylmethionine decarboxylase. Inactivat...