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1.
Enantiomeric Cyclic Peptides with Different Caco‐2 Permeability Suggest Carrier‐Mediated Transport 下载免费PDF全文
B. Sc. Eduard Puig Prof. Dr. Beat Ernst Prof. Dr. Horst Kessler 《Chemistry (Weinheim an der Bergstrasse, Germany)》2015,21(22):8023-8027
Recently, oral absorption of cyclic hexapeptides was improved by N‐methylation of their backbone amides. However, the number and position of N‐methylations or of solvent exposed NHs did not correlate to intestinal permeability, measured in a Caco‐2 model. In this study, we investigate enantiomeric pairs of three polar and two lipophilic peptides to demonstrate the participation of carrier‐mediated transporters. As expected, all the enantiomeric peptides exhibited identical lipophilicity (logD7.4) and passive transcellular permeability determined by the parallel artificial membrane permeability assay (PAMPA). However, the enantiomeric polar peptides exhibited different Caco‐2 permeability (Papp) in both directions a–b and b–a. The same trend was observed for one of the lipophilic peptide, whereas the second lipophilic enantiomer pair showed identical Caco‐2 permeability (within the errors). These findings provide the first evidence for the involvement of carrier‐mediated transport for peptides, especially for those of polar nature. 相似文献
2.
R. Weidmann 《Archiv der Mathematik》2003,81(5):589-595
We describe a family of graph manifolds that have 2-generated
fundamental group but do not admit a Heegaard splitting of genus 2. They are
closely related to the examples provided by Boileau and Zieschang if these are
considered as (non-proper) graph manifolds.Received: 14 August 2002 相似文献
3.
The ligand 2,2′,2″-nitrilotriphenol reacts with P(III) and P(V) compounds to form corresponding phosphorus complexes. Syntheses and NMR data of 2,2′,2″-nitrilotriphenyl phosphite ( II ), 2,2′,2″-nitrilotriphenyl phosphate ( III ) and of a hydrolysis product of II , 2,2′-[N-(2-hydroxyphenyl)imino]diphenly phosphonate ( IV ), are reported, as well as crystal structures of II and IV . Phosphite II shows a bicycloundecane framework; no N?Pinteraction is present. The phosphonate IV shows two coordinated and one dangling phenol group; the N-atom does not interact with the P-atom. Strong acids protonate II as well as III to form cations: in these, NMR evidence indicates coordination of the N-atom to the P-atom. 相似文献
4.
5.
Beat Jaggi Peter Mani-Levitska Bernd Sturmfels Neil White 《Discrete and Computational Geometry》1989,4(1):97-100
We give an easy general construction for uniform oriented matroids with disconnected realization space. This disproves the longstanding isotopy conjecture for simple line arrangements or order types in the plane.The research of Bernd Sturmfels and Neil White was supported in part by the Institute for Mathematics and Its Applications with funds provided by the National Science Foundation. 相似文献
6.
For the assignment of the configuration at C(8) and C(15) of the natural oviposition-deterring pheromone 1 in Rhagoletis cerasi L., the four possible stereoisomers of 1 are synthesized. By condensing the C6 building blocks (5R)- 4 and (5S)- 4 with the boron enolates of the C10 building blocks (4S)- 13 and (4R)- 13 , followed by decarboxylative dehydration, all stereoisomers of 16 are available (Scheme 5). Glucosylation of 16 followed by formation of the taurin amide gives, after deprotection, the four stereoisomers (8R,15S)- 1 , (8R,15R)- 1 , (8R,15S) -1 , and (8S,15S)- 1 (Scheme 6). 相似文献
7.
Hans Weidmann Hanns Wolf Oberwalder Egon Wildschek Helmut Schwarz 《Monatshefte für Chemie / Chemical Monthly》1972,103(1):210-217
Zusammenfassung Durch acylierende Dehydratisierung von 1,2-Isopropyliden-d-xylo-und-d-ribo-pentodialdo-furanoseoxim bzw. aus Furanuronsäureestern und-amiden werden über eine Reihe von Zwischenstufen verschiedene 3-O-Acyl-pentofuranuronsäurenitrile synthetisiert und deren Reaktionen untersucht.
Mit 1 Abbildung
Aus den DissertationenH. W. Oberwalder (1970) undE. Wildschek (1967), Technische Hochschule in Graz. 相似文献
Synthesis of xyluronic and riburonic acid derivatives
Various 3-O-acyl-pentofuranurononitrils were synthesized by acylating dehydration of 1,2-isopropylidene-d-xylo- andd-ribo-pentodialdo-furanose oximes, or pentofuranuronic acids via intermediates. Their reactions were investigated.
Mit 1 Abbildung
Aus den DissertationenH. W. Oberwalder (1970) undE. Wildschek (1967), Technische Hochschule in Graz. 相似文献
8.
13C-only spectroscopy was used to measure multiple residual (13)C-(13)C dipolar couplings (RDCs) in uniformly deuterated and (13)C-labeled proteins. We demonstrate that (13)C-start and (13)C-observe spectra can be routinely used to measure an extensive set of the side-chain residual (13)C-(13)C dipolar couplings upon partial alignment of human ubiquitin in the presence of bacteriophages Pf1. We establish that, among different broadband polarization transfer schemes, the FLOPSY family can be used to exchange magnetization between a J coupled network of spins while largely decoupling dipolar interactions between these spins. An excellent correlation between measured RDCs and the 3D structure of the protein was observed, indicating a potential use of the (13)C-(13)C RDCs in the structure determination of perdeuterated proteins. 相似文献
9.
5JHH Couplings proceeding through a HCCCCH - fragment rather than a HCOCCH - path in certain L-idofuranose derivatives are described. The probable mechanism is discussed. 相似文献
10.
Gerber B Mathys P Moser M Bressoud D Braun-Fahrländer C 《Photochemistry and photobiology》2002,76(6):664-668
It is well known that UV radiation contributes to the development of skin cancer. Exposure to solar radiation is predominantly responsible for the high incidence rate of skin cancer, but there are also indications that sunbeds are involved. The aim of the present investigation was to determine the UV emission spectra of sunbeds. It included the most common sunbed models, which cover more than 50% of the Swiss market. The UV emission spectra of sunbeds have special characteristics and are different from the sun spectrum, which can be seen in high-resolution spectral measurements. Sunbed emission spectra are similar to the sun spectrum in the UVB (280-320 nm) range but reach values 10 to 15 times higher in the UVA (320-400 nm) range. An average erythema-effective irradiance of 0.33 W/m2 was determined for sunbeds. This corresponds to a UV index of 13, which is significantly higher than the UV index of 8.5 of the high summer sun at noon at intermediate latitudes. The measurements were spread over the whole effective area of the sunbeds, and an inhomogeneous distribution of the irradiances with variations of up to 30% from the average value was found. 相似文献