- Enhancement of the Antioxidant Activity and Neurotherapeutic Features through Pyridol Addition to Tetraazamacrocyclic Molecules
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Alzheimer's and other neurodegenerative diseases are chronic conditions affecting millions of individuals worldwide. Oxidative stress is a consistent component described in the development of many neurodegenerative diseases. Therefore, innovative strategi
- Johnston, Hannah M.,Pota, Kristof,Barnett, Madalyn M.,Kinsinger, Olivia,Braden, Paige,Schwartz, Timothy M.,Hoffer, Emily,Sadagopan, Nishanth,Nguyen, Nam,Yu, Yu,Gonzalez, Paulina,Tircsó, Gyula,Wu, Hongli,Akkaraju, Giridhar,Chumley, Michael J.,Green, Kayla N.
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- Improved synthesis of symmetrically & asymmetrically: N -substituted pyridinophane derivatives
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The N,N′-di(toluenesulfonyl)-2,11-diaza[3,3](2,6)pyridinophane (TsN4) precursor was sought after as a starting point for the preparation of various symmetric and asymmetric pyridinophane-derived ligands. Various procedures to synthesize TsN4 had been published, but the crucial problem had been the purification of TsN4 from the larger 18- and 24-membered azamacrocycles. Most commonly, column chromatography or other laborious methods have been utilized for this separation, yet we have found an alternate selective dissolution method upon protonation which allows for multi-gram scale output of TsN4·HCl. This optimized synthesis of TsN4 also led to the development of symmetric RN4 derivatives as well as the asymmetric derivative N-(tosyl)-2,11-diaza[3,3](2,6)pyridinophane (TsHN4). Using this TsHN4 precursor, different N-substituents can be added to create a library of asymmetric RR′N4 macrocyclic ligands. These asymmetric RR′N4 derivatives expand the utility of the RN4 framework in coordination chemistry and the ability to study the electronic, steric, and denticity effects of these pyridinophane ligands on the metal center.
- Wessel, Andrew J.,Schultz, Jason W.,Tang, Fengzhi,Duan, Hui,Mirica, Liviu M.
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p. 9923 - 9931
(2017/12/12)
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- A NOVEL AND ECONOMICAL PROCESS FOR PREPARING (S,S)-2, 8-DIAZABICYCLO[4.3.0]NONANE AND ITS ENANTIOMER
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The present invention relates to a novel and economical process for preparing (S, S)-2, 8-diazabicyclo[4.3.0]nonane, a valuable intermediate used for constructing quinolone and naphthyridine derivatives having antibacterial effectiveness,e.g. moxifloxacin and its enantiomer.
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Page/Page column 7-8
(2008/12/07)
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- Bronchorelaxing agents based on indol- and isoquinoline derivatives
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A compound of formula (I) and its acid addition salts, wherein R1-FIj are H, lower (CrC6) alkyl; halogen; NR5R6, wherein R5, R6 are H, lower alkyl, C2-C6 acyl, SO2R7, wherein R7 is lower alkyl, CF3, aryl, substituted aryl; CN; COR8, wherein R8 is H, OH, lower alkyl, lower alkoxy; SO2R9, wherein R9 is OR10, wherein R10 is H, lower alkyl or NRnR12, wherein R11 and R12 is H or lower alkyl; ORi3, wherein R13 is H, lower alkyl, C2-C6 acyl, C1-C8 carboxy, C1-C8 carbamoyl; X is O or S; A is H, lower alkyl; B is C1-C18 alkyl optionally substituted; M is zero or 1; with the proviso that no more than three of R1-R4 are H, for treating and preventing bronchoconstructive pulmonary disease.
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Page/Page column 22-23
(2010/11/25)
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- Concave Macroheterocycles
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Macrocyclic compounds of the general type 2 having a spherical shape and a molecular cavity have been synthesized.A "fold and paste"-type cyclization step generates the macroheterocycles 4,10,11,14, and 21.Since this approach is difficult to apply for O-substituted derivatives, the "spheriphane" 24 was synthesized by intermolecular cyclization.The X-ray structure analysis of 11 shows intermolecular interactions ("dimer formation") in the crystal. Key Words: Concave molecules/ Cyclophanes/ High-dilution principle/ Macrocycles/ Spheriphanes
- Mekelburger, Hans-Bernhard,Gross, Jens,Schmitz, Juergen,Nieger, Martin,Voegtle, Fritz
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p. 1713 - 1722
(2007/10/02)
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