A rod-shaped and Gram-positive anaerobic bacterium, named Niu-O16, which was isolated from bovine rumen contents, was found to be capable of anaerobically converting isoflavones daidzein and genistein to dihydrodaidzein (DHD) and dihydrogenistein (DHG), respectively. The metabolites DHD and DHG ...
Following the thio-conjugate addition of (±)-9, its enantiomers were extremely efficiently discriminated using Novozym 435®. The thio-differentiating unit may then be removed either under reductive conditions, using Raney nickel, or following an oxidation–elimination sequence. In this manner e...
3-Acetyl-2-hydroxythiophene and 3-carbethoxy-2-hydroxythiophene have been prepared by acid-catalysed dealkylation of the corresponding t-butyl ethers at 160°. The t-butyl ethers were prepared via organometallic reagents derived from 3-bromo-2-t-butoxythiophene by metal-halogen interconversion w...
Substituted heterocycles, such as pyrrole and thiophene, are commonly found in the field of pharmaceutical and material sciences. Here we studied the reactivity of 4,5-unsubstituted alkyl 3-hydroxypyrrol-2-yl-carboxylates and 4,5-unsubstituted alkyl 3-hydroxythiophen-2-yl-carboxylates in differe...
Novel β-lactam derivatives (1c-3c) (1d-3d) were produced by using 6-aminopenicillanic acid (6-APA), 7-aminocephalosporanic acid (7-ACA) and the higher amino acid Schiff bases. The synthesized compounds were characterized by elemental analysis, IR, 1H/13C NMR and UV–vis spectra. Antibacterial a...
To develop a carrier for targeted drug delivery and triggered drug release in a reducing-tumor environment, reduction-sensitive hyaluronic acid-g-stearic acid (HCS) micelles were synthesized using a coupling agent. The HCS 40% was shown to have a more compact particle size than HCS 20% and the p...
A series of N-alkylated glycine and l-alanine bearing oligoethylene glycol (OEG) and benzyl side chains, i.e., N-(4-oligoethylene glycol)benzyl glycine and N-(4-oligoethylene glycol)benzyl alanine (NMe(OEt)xOBnG and NMe(OEt)xOBnA, x=1-3), have been readily synthesized via schiff base and reducti...
Hypochlorous acid (HClO) is an important reactive oxygen species (ROS) and plays a significant role in living organisms. Highly selective and lysosome-targetable probes for sensing hypochlorous acid are rare. In this article, we designed and prepared a new lysosome-targeting and ratiometric fluo...
Taking into consideration the eminence of 1,3-thiazoles in medicinal chemistry and in a view of procuring more pronounced biological contour, the synthesis of 2-(2-arylidenehydrazinyl)-4-arylthiazoles 6–43 was made possible by the cyclization reaction of thiosemicarbazones and α-bromoacetophen...
Wound dressing is distinctly important to wound healing, because it can not only protect wound from external disturbance, but also provide an ideal environment for wound closure. However, most of wound dressings need additional active ingredients to assist the repair process. In order to develop...
PurposeThis study aimed to investigate the properties of modified hyaluronic acid in terms of rheological properties, enzymatic degradation and mucoadhesiveness.
Octakis(2,3-di-O-methoxymethyl-6-O-tert-butyldimethylsilyl)-γ-cyclodextrin (2,3-MOM-6-TBDMS-γ-CD) was employed as stationary phase for capillary gas chromatographic separation of enantiomers. Selective introduction of the acetal function at positions 2 and 3 of the glucose units was achieved b...
The generation of a series of α-methoxymethoxy-substituted arylmethyllithiums was achieved by direct metalation of the corresponding arylmethyl methoxymethyl ethers. While the effect of substituents at the benzylic position is straightforward, substituents located on the aromatic ring promote t...
The addition of N-methoxymethyl-N-organylcarbamoyl(trimethyl)silane to α-ketoesters in anhydrous toluene at 60 °C afforded α-alkoxycarbonyl-α-siloxy amides in high yields (75–96%). The methoxymethyl was used as an amino protecting group and could be easily converted into hydrogen atom by si...
The 1,3-dithian-2-yl-methyl (Dim) and its analogous groups including dimethyl-Dim (dM-Dim) can provide a new dimension of orthogonality for carboxylic acid protection. They can be deprotected under nearly neutral oxidative conditions. In this paper, the protection of carboxylic acid with dM-Dim,...
An enantioselective C–H functionalization of N-methoxymethyl (MOM)-protected 2,3-unsubstituted indoles with α-diazopropionates has been effected via catalysis by dirhodium(II) tetrakis[N-phthaloyl-(S)-triethylalaninate], Rh2((S)-PTTEA)4, providing α-methyl-3-indolylacetates in high yields and...
The convenient transformation of acid chlorides into corresponding secondary α-ketoamides by the aminocarbonylation of acid chlorides with N-methoxymethyl-N-methylcarbamoyl(trimethyl)silane is described. The use of carbamoylsilane containing methoxymethyl group avoids the reaction of products α...
N-Methoxymethyl-N-methylcarbamoyl(trimethyl)silane reacted with N-sulfonylimines in anhydrous benzene under catalyst-free conditions to afford α-(N-sulfonyl)amino-N-methoxymethyl-N-methylamides in good to excellent yields (71–95%). Furthermore, after acid hydrolysis at room temperature, the co...
The aim of the presented study was to identify the metabolites of the new designer drug 4′-methyl-α-pyrrolidinobutyrophenone (MPBP) in rat urine using GC–MS techniques. After enzymatic hydrolysis, extraction and various derivatizations, seven metabolites of MPBP could be identified suggesting...
Three new hydroxymethyl-linked non-natural disaccharide analogues, containing an additional methylene group in between the glycosidic linkage, were synthesized by utilizing 4-C-hydroxymethyl-α-d-glucopyranoside as the glycosyl donor. A kinetic study was undertaken to assess the hydrolytic stabi...
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