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1.
Design, synthesis, and binding affinities of pyrrolinone-based somatostatin mimetics 总被引:1,自引:0,他引:1
Smith AB Charnley AK Mesaros EF Kikuchi O Wang W Benowitz A Chu CL Feng JJ Chen KH Lin A Cheng FC Taylor L Hirschmann R 《Organic letters》2005,7(3):399-402
[structure: see text] Tetrapyrrolinone somatostatin (SRIF) mimetics (cf. 1), based on a heterochiral (D,L-mixed) pyrrolinone scaffold, were designed, synthesized, and evaluated for biological activity. The iterative synthetic sequence, incorporating the requisite functionalized coded and noncoded amino acid side chains, comprised a longest linear synthetic sequence of 23 steps. Binding affinities at two somatostatin receptor subtypes (hsst 4 and 5) reveal micromolar activity, demonstrating that the d,l-mixed pyrrolinone scaffold can be employed to generate functional mimetics of peptide beta-turns. 相似文献
2.
Ion Grosu Lo?c Toupet Gerard Plé Sorin Mager Eugen Mesaros Andreea Varga Elena Bogdan 《Monatshefte für Chemie / Chemical Monthly》2000,54(5):277-286
The synthesis and stereochemistry of new dibrominated spiro-1,3-dioxane derivatives are reported. Investigations by means
of NMR methods and single crystal X-ray diffraction for two compounds revealed the high regio- and diastereoselectivity of
the bromination reaction of some new spiro-1,3-dioxanes and the asymmetric induction of the chiral carbon atom located in
the spiro skeleton. 相似文献
3.
K. Fujita A. Mesaros M.J. Lawler S. Sachdev J. Zaanen H. Eisaki S. Uchida E.-A. Kim J.C. Davis 《Physica B: Condensed Matter》2012,407(11):1859-1863
We use spectroscopic imaging scanning tunneling microscopy (SI-STM) to visualize the spatial symmetries of the electronic states that occur at the pseudogap energy scale in underdoped cuprates. We find evidence for the local intra-unit-cell electronic nematicity—by which we mean the disordered breaking of C4v symmetry within each CuO2 unit cell [1]. We also find that the coexisting incommensurate (smectic) electronic modulations couple to the intra-unit-cell nematicity through their 2π topological defects [2]. 相似文献
4.
Ion Grosu Loïc Toupet Gerard Plé Sorin Mager Eugen Mesaros Andreea Varga Elena Bogdan 《Monatshefte für Chemie / Chemical Monthly》2000,131(3):277-286
Summary. The synthesis and stereochemistry of new dibrominated spiro-1,3-dioxane derivatives are reported. Investigations by means
of NMR methods and single crystal X-ray diffraction for two compounds revealed the high regio- and diastereoselectivity of
the bromination reaction of some new spiro-1,3-dioxanes and the asymmetric induction of the chiral carbon atom located in
the spiro skeleton.
Received July 13, 1999. Accepted October 21, 1999 相似文献
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6.
The metabolism of arachidonic acid (AA) to epoxyeicosatrienoic acids (EETs) is thought to be mediated primarily by the cytochromes P450 (P450s) from the 2 family (2C9, 2C19, 2D6, and 2J2). In contrast, P450s of the 4 family are primarily involved in omega oxidation of AA (4A11 and 4A22). The ability to determine enantioselective formation of the regioisomeric EETs is important in order to establish their potential biological activities and to asses which P450 isoforms are involved in their formation. It has been extremely difficult to analyze individual EET enantiomers in biological fluids because they are present in only trace amounts and they are extremely difficult to separate from each other. In addition, the deuterium-labeled internal standards that are commonly used for stable isotope dilution liquid chromatography/mass spectrometry (LC/MS) analyses have different LC retention times when compared with the corresponding protium forms. Therefore, quantification by LC/MS-based methodology can be compromised by differential suppression of ionization of the closely eluting isomers. We report the preparation of [(13)C(20)]-EET analog internal standards and the use of a validated high-sensitivity chiral LC/electron capture atmospheric pressure chemical ionization (ECAPCI)-MS method for the trace analysis of endogenous EETs as their pentafluorobenzyl (PFB) ester derivatives. The assay was then used to show the exquisite enantioselectivity of P4502C19-, P4502D6-, P4501A1-, and P4501B1-mediated conversion of AA into EETs and to quantify the enantioselective formation of EETs produced by AA metabolism in a mouse epithelial hepatoma (Hepa) cell line. 相似文献
7.
[reaction: see text]. Diastereoselective conversion of pi-allylmolybdenum complex aldehyde 1 to organometallic triol 4 and diols 5, 10, and 13 is described. Stereocontrolled demetalation of 4, 5, and 13 was accomplished, leading to hydroxylated tetrahydrofurans and gamma-butyrolactones, as single diastereoisomers. 相似文献
8.
Stefan M. Toloman D. Popa A. Mesaros A. Vasile O. R. Leostean C. Pana O. 《Journal of nanoparticle research》2016,18(3):1-18
Journal of Nanoparticle Research - TiO2 photocatalysts co-doped with F and Fe were synthesized by a sol–gel method. Synergistic effects of F and Fe in the co-doped TiO2 were verified by NH3... 相似文献
9.
Diisopropylethylamine/hexafluoroisopropanol‐mediated ion‐pairing ultra‐high‐performance liquid chromatography/mass spectrometry for phosphate and carboxylate metabolite analysis: utility for studying cellular metabolism 下载免费PDF全文
10.
Bhat SH Gelhaus SL Mesaros C Vachani A Blair IA 《Rapid communications in mass spectrometry : RCM》2011,25(1):115-121
4‐(Methylnitrosamino)‐1‐(3‐pyridyl)‐1‐butanone (NNK) is a carcinogenic nitrosamine produced upon curing tobacco. It is present in tobacco smoke and undergoes metabolism to 4‐(methylnitrosamino)‐1‐(3‐pyridyl)‐1‐butanol (NNAL) in the lungs. NNAL undergoes further uridine diphosphate glucuronosyltransferase (UGT)‐mediated metabolism to give N‐ and O‐glucuronide metabolites, which together with free (non‐conjugated) NNAL are then excreted in the urine. The ability to conduct validated analyses of free and conjugated NNAL in human urine is important in order to assess inter‐individual differences in lung cancer risk from exposure to cigarette smoke. The use of stable isotope dilution (SID) methodology in combination with liquid chromatography/multiple reaction monitoring/mass spectrometry (LC/MRM‐MS) provides the highest bioanalytical specificity possible for such analyses. We describe a novel derivatization procedure, which results in the formation of a pre‐ionized N‐propyl‐NNAL derivative. The increased LC/MS sensitivity arising from this derivative then makes it possible to analyze free NNAL in only 0.25 mL urine. This substantial reduction in urine volume when compared with other methods that have been developed will help preserve the limited amounts of stored urine samples that are available from on‐going longitudinal biomarker studies. The new high sensitivity SID LC/MRM‐MS assay was employed to determine free and conjugated NNAL concentrations in urine samples from 60 individual disease‐free smokers. Effects of inter‐individual differences in urinary creatinine clearance on NNAL concentrations were then assessed and three metabolizer phenotypes were identified in the 60 subjects from the ratio of urinary NNAL glucuronides/free NNAL. Poor metabolizers (PMs, 14 subjects) with a ratio of NNAL glucuronides/free NNAL <2 (mean = 1.3), intermediate metabolizers (IMs, 36 subjects) with a ratio between 2 and 5 (mean = 3.4), and extensive metabolizers (EMs, 10 subjects) with a ratio >5 (mean = 11.1). Copyright © 2010 John Wiley & Sons, Ltd. 相似文献