Preparation and evaluation of cyclodextrin polypseudorotaxane with PEGylated liposome as a sustained release drug carrier

• Kayoko Hayashida,
• Taishi Higashi,
• Daichi Kono,
• Keiichi Motoyama,
• Koki Wada and
• Hidetoshi Arima

Beilstein J. Org. Chem. 2014, 10, 2756–2764, doi:10.3762/bjoc.10.292

• , phospholipids and proteins of biological membranes in the higher concentration range. Thus, CDs are utilized for studying the functions of caveolae, lipid rafts, and cholesterol transporters in various fields of cell biology [5]. Interestingly, CDs can also form inclusion complexes with linear polymers. Harada

Staudinger ligation towards cyclodextrin dimers in aqueous/organic media. Synthesis, conformations and guest-encapsulation ability

• Malamatenia D. Manouilidou,
• Yannis G. Lazarou,
• Irene M. Mavridis and
• Konstantina Yannakopoulou

Beilstein J. Org. Chem. 2014, 10, 774–783, doi:10.3762/bjoc.10.73

• and animals in vivo have been demonstrated [6]. Cyclodextrins (CDs, Scheme 1c), are cyclic oligomers of glucopyranose that act as hosts to hydrophobic molecules in aqueous environment [9][10]. CDs have been recognized as potent drug solubilizers and transporters through biological barriers with

New hydrogen-bonding organocatalysts: Chiral cyclophosphazanes and phosphorus amides as catalysts for asymmetric Michael additions

• Helge Klare,
• Jörg M. Neudörfl and
• Bernd Goldfuss

Beilstein J. Org. Chem. 2014, 10, 224–236, doi:10.3762/bjoc.10.18

• reaction of methyl acrylate with benzaldehyde the substituted triamide catalysts show a comparable or an even superior activity relative to the thiourea analogue. Recently, Gale et al. demonstrated that the same phosphoric triamides effectively act as anion transporters by hydrogen bonding [19]. These

Novel supramolecular affinity materials based on (−)-isosteviol as molecular templates

• Christina Lohoelter,
• Malte Brutschy,
• Daniel Lubczyk and
• Siegfried R. Waldvogel

Beilstein J. Org. Chem. 2013, 9, 2821–2833, doi:10.3762/bjoc.9.317

• ][34], compounds based on (−)-isosteviol have found application in various fields of synthetic chemistry [35], including the construction of tweezer-like supramolecular transporters for amino acids [36], chiral organocatalysts in aldol reactions [37], or the complex formation with aromatic compounds

Synthesis and characterization of novel bioactive 1,2,4-oxadiazole natural product analogs bearing the N-phenylmaleimide and N-phenylsuccinimide moieties

• Catalin V. Maftei,
• Elena Fodor,
• Peter G. Jones,
• M. Heiko Franz,
• Gerhard Kelter,
• Heiner Fiebig and
• Ion Neda

Beilstein J. Org. Chem. 2013, 9, 2202–2215, doi:10.3762/bjoc.9.259

• transport in cells by using natural transporters such as amino acids, peptides or sugars. Moreover, it is desirable to reduce, or even remove completely, the secondary effects to minimize the toxicity and increase the selectivity. All derivatives were obtained with a high purity (at least 97% based on 1H

Flow synthesis of a versatile fructosamine mimic and quenching studies of a fructose transport probe

• Matthew B. Plutschack,
• D. Tyler McQuade,
• Giulio Valenti and
• Peter H. Seeberger

Beilstein J. Org. Chem. 2013, 9, 2022–2027, doi:10.3762/bjoc.9.238

• the pancreatic islets and hepatic cells of people with diabetes, which may explain glucose insensitivity and the progression of non-alcoholic fatty liver disease [6][7]. Passive carbohydrate transporters are well-known targets for carbohydrate-based probes [8]. The positron emission tomography (PET

Recent progress in the discovery of small molecules for the treatment of amyotrophic lateral sclerosis (ALS)

• Allison S. Limpert,
• Margrith E. Mattmann and
• Nicholas D. P. Cosford

Beilstein J. Org. Chem. 2013, 9, 717–732, doi:10.3762/bjoc.9.82

• patients. The actions of glutamate, the primary excitatory neurotransmitter in the nervous system, are terminated by the uptake of glutamate away from the synapse by numerous glutamate transporters [15]. In particular, the Na+-dependent excitatory amino acid transporter 2 (EAAT2), which is present on glial

A chemist and biologist talk to each other about caged neurotransmitters

• Graham C.R. Ellis-Davies

Beilstein J. Org. Chem. 2013, 9, 64–73, doi:10.3762/bjoc.9.8

• functionality cannot give rise to such undesirable effects. However, at low concentrations (range 5–300 µM) it seems that these off-target effects are significantly reduced [38][39]. For other glutamate receptors, such as amino acid transporters involved in the clearance of glutamate by astrocytes, caged

Synthesis of 5-oxyquinoline derivatives for reversal of multidrug resistance

• Torsten Dittrich,
• Nils Hanekop,
• Nacera Infed,
• Lutz Schmitt and
• Manfred Braun

Beilstein J. Org. Chem. 2012, 8, 1700–1704, doi:10.3762/bjoc.8.193

• 10.3762/bjoc.8.193 Abstract The inhibition of ABC (ATP binding cassette) transporters is considered a powerful tool to reverse multidrug resistance. Zosuquidar featuring a difluorocyclopropyl-annulated dibenzosuberyl moiety has been found to be an inhibitor of the P-glycoprotein, one of the best-studied

• “multidrug resistance”. Various transporters of the ATP-binding cassette family, so called ABC transporters, have been shown to be responsible for multidrug resistance [1]. Among these multidrug-resistance ABC transporters, the P-glycoprotein has been investigated most intensively [2]. As P-glycoprotein is

• the reference compound zosuquidar (1a) was determined for the ABC transporters LmrCD and Pdr5. The results are given in Table 1, which restricts itself to those compounds that displayed a significantly enhanced activity compared to that of 1a. The activity of the individual transporters in the absence

Mutational analysis of a phenazine biosynthetic gene cluster in Streptomyces anulatus 9663

• Orwah Saleh,
• Katrin Flinspach,
• Lucia Westrich,
• Andreas Kulik,
• Bertolt Gust,
• Hans-Peter Fiedler and
• Lutz Heide

Beilstein J. Org. Chem. 2012, 8, 501–513, doi:10.3762/bjoc.8.57

• subunits of cytochrome d ubiquinol oxidase, and ppzR1 and ppzR2 to ABC transporters. The next gene, orf12, shows very high similarities to the primary metabolic enzyme allantoicase (allantoate amidohydrolase, EC 3.5.3.4), an enzyme of purine catabolism. It is separated from ppzR2 by a gap of 1.3 kb and

• ; production of nonprenylated phenazines was similar in both strains. The most likely explanation of this result is that the ABC transporters encoded by ppzR1 and ppzR2 are involved in the export of endophenazines, and therefore their inactivation reduces but does not completely prevent the production of these

• gene cluster comprises the 27 kb DNA region stretching from the phenazine prenyltransferase gene ppzP to the ABC transporters ppzR1 and ppzR2. Inactivation experiments provided initial genetic insights into the regulation of phenazine biosynthesis in Streptomyces. While the complicated network