Dendroaspis natriuretic peptide (DNP), recently isolated from the venom of the green Mamba snake Dendroaspis angusticeps, is a 38 amino acid peptide containing a 17 amino acid disulfide ring structure similar to that of the natriuretic peptide family. The natriuretic peptide family is known to i...
The involvement of spinal release of histamine on nociceptive behaviors induced by spermine was examined in mice. Intrathecal spermine produced dose-dependent nociceptive behaviors, consisting of scratching, biting and licking. The nociceptive behaviors induced by spermine at 0.02 amol and 10 pm...
Venom of the Australian ant species Myrmecia pilosula contains a number of allergenic peptides including pilosulins. To obtain novel cDNA clones that encode the pilosulin-related bioactive peptides, mRNA of M. pilosula species complex was subjected to RT-PCR in which the forward primer correspon...
Albumin, the most abundant plasma protein, readily enters sites of inflammation during the period of increased vascular permeability. There it encounters proteases released from mast cells and invading leukocytes which earlier work has shown can act on albumin to liberate the peptide, histamine ...
Kinetic modeling of gas-phase synthesis of ethyl chloride from ethanol and hydrochloric acid over high porous Al2O3 and 2 wt% ZnCl2/Al2O3 catalysts was studied in a continuous plug flow reactor in the temperature range of 200–325 °C. Two rival kinetic models were proposed that both describe th...
Low permeability of microbial cells and mass transfer limitations are major problems for efficient whole-cell biocatalysis. In this work, a method for enhanced enantioselective synthesis of S-EHPP, an intermediate for antidepressant drug fluoxetine via Kluyveromyces lactis whole-cell-catalyzed r...
The corrosion inhibition behavior of 1-ethyl 3-methylimidazolium thiocyanate, (EMIM)+(SCN)− ionic liquid (IL), on API 5 L X52 steel immersed in 0.5 M H2SO4 and 0.5 M HCl aqueous solutions were studied. The kinetic corrosion parameters were determined using a gravimetrical method and electrochemi...
The synthesis of novel 2H-benzo[b][1,4]oxazin-3(4H)-one derivatives has been carried out using trifluoroacetic anhydride/phosphoric acid mediated C–C bond forming reaction as a key step. This method does not require the use of environmentally harmful AlCl3 or moisture sensitive acid chloride. A...
An efficient preparation of multisubstituted benzimidazoles and quinoxalin-2(1H)-ones by Ugi 4CC/aza-Wittig sequence was developed. The 2-azidobenzenamines, obtained from CH activation of aromatic amine precursors, reacted with aldehydes, acids, and isocyanides to produce Ugi products, which wer...
Resveratrol (3,5,4′-trihydroxylstilbene) has been proposed to elicit a variety of positive health effects including protection against cancer and cardiovascular disease. The highest affinity target of resveratrol identified so far is the oxidoreductase enzyme quinone reductase 2 (QR2), which is...
Thirty (1E,4E,6E)-1,7-diaryl-1,4,6-heptatrien-3-ones, featuring a central linear trienone linker and two identical nitrogen-containing heteroaromatic rings, were designed and synthesized as curcumin-based anticancer agents on the basis of their structural similarity to the enol-tautomer of curcu...
Aryl-substituted α,β-difluoroallyl alcohols 1 were readily hydrolyzed in the presence of a catalytic amount of montmorillonite K 10 (clay) in hexane at reflux temperature for 1 h to give the corresponding (Z)-α-fluoro-β-aryl-substituted acrylaldehydes 2 in good yields.
A series of chiral 1,3-aminoalcohols derived from cis-(1R,2S)-2-benzamidocyclohexanecarboxylic acid were synthesized and applied to the enantioselective arylation of aromatic aldehydes. The reactions exhibited good yields (up to 90%) and moderate to high enantioselectivities (up to 99%). Not onl...
Nine novel 6-fluorothymine nucleoside analogues of both N(1)-α/β and N(3)-β-ribo series were prepared by the Vorbrüggen method starting from persilylated 6-fluorothymine and 1-O-acetyl-2,3,5-tri-O-benzoyl-β-d-ribofuranose, 1-O-acetyl-2,5-di-O-benzoyl-3-deoxy-3-fluoro-α,β-d-ribofuranose or...
Both enantiomers of 2-acetoxymethyl-1-hydroxymethylferrocene have been obtained via enantiotoposelective irreversible acylation in organic medium of 1,2-bis(hydroxymethyl)ferrocene using vinyl acetate as acyl donor and a lipase as catalyst.
2,3-bis(acetoxymethyl)bicyclo[2.2.1]hepta-2,5-diene 1 undergoes nucleophilic attack of secondary amines under catalyzed Pd(0) reaction conditions. The influence of various tertiary amines as acceptor bases on the reaction as well as the nature of the organophosphorus ligands on the metal has bee...
(2R, 3S)-2-Acetoxymethyl-3-hydroxymethylazirizines of high enantiomeric purity were prepared through enzymatic transesterification of meso-bis(acetoxymethyl)aziridines.
Pseudomonas fluorescens lipase (PFL)-catalyzed asymmetric hydrolysis of meso-2,5-bis(acetoxymethyl)-3,4-(isopropylidenedioxy)tetrahydrofuran 3 afforded the optically active monoacetate (−)-7 of high enantiomeric excess (92% ee) in 94% yield. Transesterification of meso-bis(hydroxymethyl)-3,4-(is...
Two efficient, metal free reagent systems, PhI(OAc)2-I2 (method A) and IBX-I2 (method B), for stereoselective synthesis of trans-2-deoxy-2-iodoglycosylacetates and O-iodobenzoates respectively from differently protected glycals have been developed. They are compatible with a variety of protectin...
meso-Bis(acetoxymethyl)-1,4,5,6,7,7-hexachlorobicyclo[2.2.1]hepta-2,5-diene and meso-bis(hydroxymethyl)-1,4,5,6,7,7-hexachlorobicyclo[2.2.1]hepta-2,5-diene were transformed into chiral monoesters with 65–92% ee via enzymatic desymmetrization using various lipases. The absolute configuration was...
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