72631-59-5Relevant academic research and scientific papers
Novel bacterial topoisomerase inhibitors derived from isomannide
Okumu, Antony,Lu, Yanran,Dellos-Nolan, Sheri,Papa, Jonathan L.,Koci, Bryan,Cockroft, Nicholas T.,Gallucci, Judith,Wozniak, Daniel J.,Yalowich, Jack C.,Mitton-Fry, Mark J.
, (2020)
A series of Novel Bacterial Topoisomerase Inhibitors (NBTIs) employing a linker derived from isomannide were synthesized and evaluated. Reduced hERG inhibition was observed compared to structure-matched analogues with different linkers, and compound 6 showed minimal proarrhythmic potential using an in vitro panel of cardiac ion channels. Compound 6 also displayed excellent activity against fluoroquinolone-resistant MRSA (MIC90 = 2 μg/mL) and other Gram-positive pathogens.
BACTERIAL TOPOISOMERASE INHIBITORS DERIVED FROM ISOMANNIDE
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Page/Page column 33; 34, (2021/07/31)
Disclosed are bacterial topoisomerase inhibitors employing a linker derived from isomannide. Reduced hERG inhibition was observed compared to structure-matched analogues with different linkers.
Synthesis of 2-[18F]Fluoro-2-deoxyisosorbide 5-mononitrate and Assessment of Its in vivo Biodistribution as Determined by Dynamic Positron Emission Tomography (PET)
Santschi, Nico,Wagner, Stefan,Daniliuc, Constantin,Hermann, Sven,Sch?fers, Michael,Gilmour, Ryan
, p. 1724 - 1732 (2015/10/06)
Herein we disclose the synthesis of 2-fluoro-2-deoxyisosorbide 5-mononitrate (2F-IS-5MN), a fluorinated analogue of the commonly prescribed vasodilator isosorbide 5-mononitrate (IS-5MN). X-ray structural data for IS-5MN and its C2-epimeric congener IM-5MN are presented together with structural data for 2F-IS-5MN. Radioisotope labeling of 2F-IS-5MN has, for the first time, allowed observation of the in vivo biodistribution of this organic nitrate by means of dynamic positron emission tomography (PET) in wild-type mice. Visualization breakthrough: Herein we disclose the synthesis of a fluorinated analogue of the commonly prescribed vasodilator isosorbide 5-mononitrate (IS-5MN). Radioisotope labeling of 2F- IS-5MN has, for the first time, allowed observation of the in vivo biodistribution of this organic nitrate by means of dynamic positron emission tomography (PET) in wild-type mice.
MONOFLUORINATED DERIVATIVES OF DIANHYDROHEXITOLS AND PROCESSES FOR MAKING THE SAME
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Paragraph 0041; 0042, (2014/01/08)
Novel monofluoro analogs of isosorbide, isomannide and isoidide are described, together with processes for making such monofluoro analogs.
Novel peptide mimetics based on N-Protected amino acids derived from isomannide as potential inhibitors of NS3 serine protease of hepatitis C virus
Barros, Thalita G.,Zorzanelli, Bruna C.,Pinheiro, Sergio,De Brito, Monique A.,Tanuri, Amilcar,Da Costa, Emmerson C.B.,Mohana-Borges, Ronaldo S.,Rodrigues, Carlos R.,Souza, Alessandra T.M.,Ferreira, Vitor F.,Muri, Estela M.F.
experimental part, p. 239 - 249 (2012/07/27)
Abstract: Hepatitis C virus (HCV) is among the most important flaviviruses. It has a serine protease which is important for viral replication and this enzyme constitutes a suitable target for new anti-retroviral drugs. Herein we disclose a series of amide and ester peptide mimetic inhibitors of serine proteases, all of them obtained via coupling reactions of isomannide derivatives with N-protected amino acids. The arginine derivative 19 showed 45% of inhibition of NS3/4A serine protease at 100 μM and molecular modeling studies had shown that 19 interacted with the active site of this enzyme.
New chiral imidazolium ionic liquids from isomannide
Gomes Da Silva,Pereira, M. Manuela A.
body text, p. 197 - 202 (2011/03/18)
New chiral bis and mono-imidazolium ionic liquids derived from isomannide were synthesized. The structural features of the chiral organic cations impart a special arrangement of the chiral cavity. The new chiral chloride salts of isomannide derivatives ar
Copper-Catalyzed vs thermal step growth polymerization of starch-derived α-w-alkyne dianhydrohexitol stereoisomers: to click or not to click?
Besset, Celine,Binauld, Sandra,Ibert, Mathias,Fuertes, Patrick,Pascault, Jean-Pierre,Fleury, Etienne,Bernard, Julien,Drockenmuller, Eric
scheme or table, p. 17 - 19 (2011/09/14)
The synthesis of α-azide-ω-alkyne 1,4:3,6-dianhydrohexitols with controlled stereochemistry from starch-derived isosorbide, isomannide, and isoidide as well as a detailed study of their polyaddition by CuAAC in solution or by catalyst and solvent-free 1,3
TETRAHYDROFURO [3, 2-B] PYRROL-3-ONE DERIVATIVES AS INHIBITORS OF CYSTEINE PROTEASES
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Page/Page column 82-83, (2009/12/27)
A compound of formula (I), or a pharmaceutically acceptable salt, hydrate, complex or pro-drug thereof, wherein one of R1 and R2 is H, and the other is selected fromC1-8-alkyl, C3-6-cycloalkyl and C1-8/sub
Stereospecific method for the preparation of dioxa-bicyclooctane compounds
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Page/Page column 10-11, (2009/12/27)
This invention relates to a new method for the stereospecific thiocarboxylation of organic compounds for the preparation of compounds according to formula (I): wherein a compound of formula (II): is reacted with a compound of formula (IIIa) or (IIIb): the
