73111-13-4Relevant academic research and scientific papers
A new way to do an old reaction: highly efficient reduction of organic azides by sodium iodide in the presence of acidic ion exchange resin
Suthagar, Kajitha,Fairbanks, Antony J.
supporting information, p. 713 - 715 (2017/01/13)
Organic azides are readily reduced to the corresponding amines by treatment with sodium iodide in the presence of acidic ion exchange resin. The process, optimal when performed at 40 °C and 200 mbar pressure on a rotatory evaporator, is extremely efficient, clean, and tolerant of a variety of functional groups.
Evaluation of potential Myt1 kinase inhibitors by TR-FRET based binding assay
Rohe, Alexander,Goellner, Christiane,Wichapong, Kanin,Erdmann, Frank,Al-Mazaideh, Ghassab M.A.,Sippl, Wolfgang,Schmidt, Matthias
, p. 41 - 48 (2013/04/23)
In the human cell cycle, the Myt1 kinase is a crucial regulator of the G2/M transition. Because this membrane-associated kinase is hard to obtain and assay, there is a distinct lack of data so far. Here we report the derivatization of a glycoglycerolipid which was shown previously to be active in a Myt1 activity assay. These compounds were tested in a binding assay together with a set of common kinase inhibitors against a full-length Myt1 expressed in a human cell line. Dasatinib exhibited nanomolar affinity whereas broad coverage inhibitors such as sunitinib and staurosporine derivatives did not show any effect. We also carried out docking studies for the most potent compounds allowing further insights into the inhibitor interaction of this kinase. The glycoglycerolipids showed no significant effects in the binding assay, endorsing the idea of a mechanism of action distant from the active site.
Synthesis of non-glycosidically linked selenoether pseudodisaccharides
Fournière, Viviane,Cumpstey, Ian
supporting information; experimental part, p. 2127 - 2129 (2010/06/14)
Non-glycosidically linked disaccharide mimetics with a selenoether functionality linking the two monosaccharide residues have been synthesised. Protected Glc(Se3-3)Glc, Glc(Se3-6)Glc and Glc(Se3-6)Man structures were obtained. Selenium was introduced by d
First total synthesis of 1,2-dipalmitoyl-3-(N-palmitoyl-6′-amino-6′-deoxy-α-d-glucosyl)-sn-glycerol-a glycoglycerolipid of a marine alga with a high inhibitor activity against human Myt1-kinase
Goellner, Christiane,Philipp, Claudia,Dobner, Bodo,Sippl, Wolfgang,Schmidt, Matthias
scheme or table, p. 1628 - 1631 (2009/12/09)
The first total synthesis of 1,2-dipalmitoyl-3-(N-palmitoyl-6′-amino-6′-deoxy-α-d-glucosyl)-sn-glycerol, a glycoglycerolipid isolated from a marine alga extract, is described. Starting from α-methylglucopyranoside the multistep strategy allows the stereoselective synthesis of the final compound using various protective group procedures as well as derivatization of partial molecule domains. The latter offers the development of lead structures for inhibitors of human Myt1-kinase.
Synthesis of new sugar-based surfactants and evaluation of their hemolytic activities
Neimert-Andersson, Kristina,Sauer, Sven,Panknin, Olaf,Borg, Tessie,Soederlind, Erik,Somfai, Peter
, p. 3623 - 3626 (2007/10/03)
The synthesis of four sugar-based surfactants derived from glucose and (R)-12-hydroxystearic acid is described. The surfactants have a hydroxy group in the hydrophobic part, which is either free or acylated using acetyl chloride, hexanoyl chloride, or myristoyl chloride. Three of the synthesized surfactants are water-soluble and are evaluated with respect to their CMCs and hemolytic activities. The fourth surfactant has limited water solubility and is not further included in the study. The investigated surfactants are all hemolytic close to their respective CMC indicating that their use in parenteral formulations may be limited. Nevertheless, surfactants having the proposed structure appear as promising alternatives to existing solubilizing agents for pharmaceutical applications.
Carbohydrate sulfonyl chlorides for simple, convenient access to glycoconjugates
Kvaerno, Lisbet,Werder, Moritz,Hauser, Helmut,Carreira, Erick M.
, p. 1145 - 1148 (2007/10/03)
(Chemical Equation Presented) The use of carbohydrate sulfonyl chlorides is introduced as a new, facile glycoconjugation method which could find broad applications. We demonstrate the approach by synthesizing a number of glycosylated cholesterol absorptio
Synthesis and in vitro evaluation of inhibitors of intestinal cholesterol absorption
Kv?rn?, Lisbet,Werder, Moritz,Hauser, Helmut,Carreira, Erick M.
, p. 6035 - 6053 (2007/10/03)
We have utilized our recently developed in vitro assay to address two key questions in the design of small-molecule cholesterol absorption inhibitors using ezetimibe, the only drug yet approved for the inhibition of cholesterol absorption in the small int
Novel hypocholesterolemic compounds
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Page/Page column 15-16, (2008/06/13)
The present invention relates to novel hypocholesterolemic compounds of formula I useful in the treatment and prevention of atherosclerosis and for the reduction of cholesterol levels as well as to pharmaceutical compositions comprising said compounds alo
Synthesis of biomimetic analogs of neomycin B: Potential inhibitors of the HIV RNA Rev response element
Nishizono, Naozumi,Nair, Vasu
, p. 283 - 295 (2007/10/03)
The aminoglycosidic antibiotic, neomycin B, is an inhibitor of the binding of Rev to RRE. This paper reports on the synthesis of analogs of neomycin B as potential anti-HIV compounds designed to function as inhibitors of Rev/RRE binding.
SYNTHESIS OF AMYLOSTATIN (XG), α-GLUCOSIDASE INHIBITOR WITH BASIC PSEUDOTRISACCHARIDE STRUCTURE
Sakairi, Nobuo,Kuzuhara, Hiroyoshi
, p. 5327 - 5330 (2007/10/02)
The basic pseudotrisaccharide (1) constituting the common and essential building block of several α-glucosidase inhibitors of microbial origin was synthesized by coupling two synthons: the chiral cyclohexyl halide (11) and the 4'-amino-4'-deoxy-disaccharide (14).
