Secretin, a 27-amino-acid peptide hormone produced by intestinal S cells, is released into the duodenum primarily in response to pH changes following food ingestion. Its major target organs include the pancreas, stomach, and gallbladder. Secretin affects pancreatic bicarbonate secretion, gastric...

Most theories of meal-induced thermogenesis involve a gut-brain-brown adipose tissue axis driving sympathetic nervous system-mediated thermogenesis. Li et al. demonstrate that secretin released by the gut after a meal binds to abundant receptors in brown adipose tissue to stimulate thermogenesis...

PurposeTo investigate whether jejunal secretions are independent of the pancreatic response to secretin in secretin-enhanced Magnetic Resonance Cholangiopancreatography (s-MRCP) examination of subjects with and without chronic pancreatitis (CP).

SummaryThe molecular mediator and functional significance of meal-associated brown fat (BAT) thermogenesis remains elusive. Here, we identified the gut hormone secretin as a non-sympathetic BAT activator mediating prandial thermogenesis, which consequentially induces satiation, thereby establish...

Based on the structure of the active site of cytochrome P450 14α-demethylase (CYP51) and the conclusions of the structure-activity relationships of azole antifungals, a series of 1-(2-(2,4-difluoro-phenyl)-2-hydroxy-3-(1H-1,2,4-triazol-1-yl)propyl)-1H-1,2,4-triazol-5(4H)-one of fluconazole anal...

The 12-(3'hydroxy-n-propyl)-deoxoartmisinin was synthesized from artemisinic acid via photooxidative cyclization as a key step. The title compound 6a is found to show five times greater in vitro antimalarial acitivity compared to artemisinin.

Three novel neostigmine bromide (NEO) selective electrodes were investigated with 2-nitrophenyl octyl ether as a plasticiser in a polymeric matrix of polyvinyl chloride (PVC). Sensor 1 was fabricated using tetrakis(4-chlorophenyl)borate (TpClPB) as an anionic exchanger without incorporation of a...

Newly developed acyclic nucleoside phosphonates, derivatives of adenine and 2,6-diaminopurine bearing the 2-hydroxy-3-(phosphonomethoxy)propyl (HPMP) moiety at the N9-side chain (i.e., HPMPA and HPMPDAP, respectively) were screened for in vitro immunobiological activity, using mouse resident per...

Synthesis, characterization, resolution and evaluation of novel (R/S)-2-[2-hydroxy-3-(4-phenylpiperazin-1-yl)propyl]-1H-pyrrolo[3,4-b]quinolin-3(2H)-one derivatives are described. Enantiomerically pure compounds were isolated in good to excellent yield with high enantiomeric excess under mild re...

Natural β-cyclodextrin (cyclomaltoheptaose) was treated with sodium hydride and allyl bromide to form the per-O-allyl-β-cyclodextrin. 9-BBN, sodium hydroxide and hydrogen peroxide were then added to form, after adequate treatments, the desired per-O-(3-hydroxy)propyl-β-cyclodextrin in yields ...

A series of 2-(2,4-difluorophenyl)-2-hydroxy-3-(1H-1,2,4-triazol-1-yl)propyl dithiocarbamates as new analogs of fluconazole were synthesized and their antifungal activities were evaluated. Among these compounds, 2a–f and 3a–q exhibited higher activities than fluconazole against nearly all fung...

A series of N-(2-hydroxy)propyl-3-trimethyl ammonium chitosan chloride (HTCC) samples with various degrees of quaternization ranging from 12.4 to 43.7% was synthesized. The structures and properties of HTCC were investigated by FT-IR, 1H NMR, conductometric titration and XRD analysis. It was fou...

We report here the synthesis, characterization of seventeen (E)-2-methyl-3-ferrocenyl-N-acrylamides. The single crystal structures of the key intermediate b and two target compounds d5 and d6 were confirmed by X-ray crystallographic analysis. Antitumor activity of all compounds was tested in vit...

A novel and efficient TBHP/TBAI-mediated oxidation of thiophenols is described. The reactions proceeded smoothly to give tert-butyl arylsulfinates in up to 82% yield with good functional group compatibility under mild conditions.

CuI/trans-4-hydroxy-l-proline catalyzed coupling of aryl iodides with tert-butyl β-keto esters proceeded smoothly at 40 °C in DMF, providing α-aryl ketones after acid-promoted deprotection and decarboxylation of tert-butyl ester group. While CuI/2-picolinic acid catalyzed coupling of aryl iod...

A general method is presented for the preparation of tert-butyl esters by the gentle warming of the carboxylic acid in the presence of excess of tert-butyl acetoacetate and a catalytic amount of acid. This method generates only low pressures, and is therefore suitable for laboratory scale pressu...

Alternating conventional radical copolymerization of tert-butyl-2-trifluoromethacrylate (a non-homopolymerizable fluoromonomer under radical conditions) with vinyl acetate, initiated by 2,2′-azo-bis(4-methoxy-2,4-dimethyl valeronitrile) at 40 °C is presented. The study of the kinetics of the c...

Enantioselective aldol reactions between ketones and aldehydes were shown to be catalysed by a variety of tert-butyl esters of peptides. Amongst the peptides tested, Pro-Glu(OtBu)-OtBu proved to be the best, affording the product in good to excellent yields, diastereoselectivities and enantiosel...

Poly(ethylene phosphoric acid)s (PEPA)s of different compositions, namely homopolymers, and diblock and triblock copolymers containing poly(ethylene glycol) monomethyl ether, l-lactide, and ε-caprolactone blocks, can be quantitatively obtained by mild thermolysis of polymers based on tert-butyl...

The very common protection reactions of scaffolds by introduction of Boc or tert-butyl groups on lactams or acids in the pyroglutamic series have been revisited in a green perspective. Particularly, reaction conditions allowing a quantitative yield in substitution of bromine in tert-butyl bromid...