Ethyl (R)-2-hydroxy-4-phenylbutyrate ((R)-HPBE), a key intermediate in the production of angiotensin-converting enzyme (ACE) inhibitors, was prepared by the microbial reduction of ethyl 2-oxo-4-phenylbutyrate (OPBE). Among 63 microorganisms tested, Candida krusei SW2026, for the first time, was ...
Ethyl (R)-2-hydroxy-4-phenylbutanoate [(R)-HPBE] is a versatile and important chiral intermediate for the synthesis of angiotensin-converting enzyme (ACE) inhibitors. Recombinant E. coli strain coexpressing a novel NADPH-dependent carbonyl reductase gene iolS and glucose dehydrogenase gene gdh f...
(Liquid–liquid) equilibrium (LLE) data of the solubility curves and tie-line compositions have been determined for mixtures of (water + 3-hydroxy-2-butanone + ethyl ethanoate) at 298.15 K, 308.15 K and 318.15 K and 101.3 kPa. Distribution coefficients and separation factors have been evaluated ...
A new biocatalytic strategy to obtain the ethyl (R)-2-hydroxy-4-oxo-4-phenylbutyrate precursor of ethyl (R)-2-hydroxy-4-phenylbutyrate, an important intermediate in the synthesis of a variety of ACE inhibitors, has been set up. Starting from ethyl 2,4-dioxo-4-phenylbutyrate, a screen of microorg...
Recombinant strains of Pichia pastoris expressing carbonyl reductase CgKR2 from Candida glabrata were constructed for stereoselective reduction of ethyl-2-oxo-4-phenylbutyrate (OPBE) to ethyl (R)-2-hydroxy-4-phenylbutyrate [(R)-HPBE], an important building block for synthesis of angiotensin-conv...
The treatment of 2-[(1-alkyl(aryl)-4-cyano-5,6,7,8-tetrahydroisoquinolin-3-yl)oxy]acetamides (5) with sodium ethoxide to induce a cyclization to form 5-alkyl(aryl)-1-amino-6,7,8,9-tetrahydrofuro[2,3-c]isoquinoline-2-carboxamides 4 furnished unexpected results. Compounds 5 gave rise to two differ...
An effective method for the synthesis of 3,4-disubstituted quinolin-2(1H)-ones was reported. α-Carbonylalkyl radical, produced by the manganese(III) acetate oxidation of α-substituted N-[2-(phenylethynyl)phenyl]acetamides, undergoes a 6-exo-dig cyclization onto the C–C triple bond efficiently...
A series of thiobarbituric acid derivatives 1–27 were synthesized and evaluated for their urease inhibitory potential. Exciting results were obtained from the screening of these compounds 1–27. Compounds 5, 7, 8, 11, 16, 17, 22, 23 and 24 showed excellent urease inhibition with IC50 values 18....
Biological evaluation of 3,4-dihydroxy piperidines as α-glucosidase inhibitors is being reported for the first time. Forty-five derivatives (amides, di-amides and sulfonamides) were made using cis and trans 3,4-dihydroxy piperidines to evaluate their α-glucosidase inhibition activity. Polar gr...
The molecular structure of the microcomponents of olive fruit was investigated in order to evidence new molecules which could be transferred to the resulting oil and therefore be typical of olive oil. The three glucosides of 2(3,4-dihydroxy-phenyl)ethanol, 1, 2 and 3 were isolated together with ...
A number of novel indomethacin glycolamide esters were synthesized and tested for their cyclooxygenase (COX-1 and COX-2) inhibition properties in vitro. Many of these compounds proved to be selective COX-2 inhibitors, and subtle structural changes in the substituents on the glycolamide ester moi...
Four layers of horizontal cell could be identified in the carp retina, among which three were revealed under photopic condition by means of procion yellow injection. From receptor side they are designated the outermost (Layer I), the outer (Layer II) and the inner (Layer III) horizontal cell lay...
Aspartate transcarbamoylase from wheat germ is irreversibly inactivated by the triazinyl dye Procion Red HE3B. Since triazinyl dyes may mimic nucleotides, and UMP is a known allosteric modifier of this enzyme, the reaction was studied to elucidate whether the dye is an ‘affinity label’ for the...
The residual defatted biomass (RDB) of the fungus Nigrospora sp. obtained from the oil extraction process using supercritical technology was used as a low cost biosorbent for the removal of Procion red H–E7B dye (PR H–E7B) from aqueous solutions. The biosorption was favored using a biosorbent ...
Pearl powder, a well-known traditional mineral medicine, is reported to be used for well-being and to treat several diseases from centuries in Taiwan and China. We investigated the in vitro antihemolytic and antioxidant properties of pearl powder that could protect erythrocytes against 2,2′-azo...
The aim of this study was to analyze the effect of AAPH on the conformational structure and allergenicity of shrimp tropomyosin (TM). The structure of AAPH-TM was evaluated by SDS-PAGE, fluorescence, circular dichroism (CD) and ultraviolet light (UV), and the allergenicity was evaluated by in vi...
Trichomonas vaginalis (T. vaginalis) is a common sexually transmitted infection, affecting the urogenital tract. Trichomoniasis is customarily treated with metronidazole (MTZ). MTZ is known to cause undesirable side effects and there is several reports on MTZ resistant T. vaginalis. Thus, the pr...
A facile synthesis for 1-fluoro-3-(trifluoromethyl)adamantane, based on fluorination of 3-hydroxyadamantane-1-carboxylic acid, was developed. Its synthetic potentialities for preparation of (trifluoromethyl)adamantane derivatives containing diverse functional groups (acids, amines, etc.) in a br...
A series of short axially symmetrically 1,3,6,8-tetrasubstituted pyrene-based derivatives (4a–4c) with two 4-tert-butylphenyl segments at 1,8-positions and two hole-transporting arylamine attachments at 3,6-sites of pyrene core were designed and synthesized based on stepwise synthetic strategy....
Three novel europium complexes with 1-(4-tert-butylphenyl)-3-(2-naphthyl)-propane-1,3-dione (TNPD) and 2,2-dipyridine (Bipy) or 1,10-phenan-throline (Phen) were synthesized and confirmed by FT-IR, 1H NMR, UV–vis absorption and elemental analysis. Photoluminescence behavior of complexes Eu(TNPD)...
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