Recent Advances in the Synthesis of Piperazines: Focus on C–H Functionalization
Organics, 2021 Piperazine ranks as the third most common nitrogen heterocycle in drug discovery, and it is the key component of several blockbuster drugs, such as Imatinib (also marketed as Gleevec) or Sildenafil, sold as Viagra.
Carolina Durand, Michal Szostak
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Synthesis of Chromeno[3,4-b]piperazines by an Enol-Ugi/Reduction/Cyclization Sequence
Molecules, 2021 Keto piperazines and aminocoumarins are privileged building blocks for the construction of geometrically constrained peptides and therefore valuable structures in drug discovery.
Ana Bornadiego +2 more
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Derivatives of Piperazines as Potential Therapeutic Agents for Alzheimer’s Disease [PDF]
Molecular Pharmacology, 2019 Alzheimer’s disease (AD) is a neurodegenerative disorder that is the major cause of dementia in the elderly. There is no cure against AD. We have recently discovered a novel transient receptor potential canonical 6 (TRPC6)–mediated intracellular ...
Елена Попугаева +8 more
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Stereoselective electrochemical intramolecular imino-pinacol reaction: a straightforward entry to enantiopure piperazines [PDF]
Beilstein Journal of Organic ChemistryThe stereoselective electroreductive intramolecular coupling of chiral diimines of aromatic aldehydes with trans-1,2-diaminocyclohexane for the synthesis of enantiopure tetrasubstituted piperazines has been investigated by an electrochemical approach ...
Margherita Gazzotti +5 more
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CO2 Capture with Silylated Ethanolamines and Piperazines
ChemistryOpen, 2020 Invited for this month's cover is the group of Marcus Herbig from the TU Bergakademie in Freiberg. The cover picture shows the reaction of CO2 with a silyl derivative of the biogenic amine ethanolamine.
Marcus Herbig +5 more
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Alkylated Piperazines and Piperazine-Azole Hybrids as Antifungal Agents [PDF]
Journal of Medicinal Chemistry, 2017 The extensive use of fluconazole (FLC) and other azole drugs has caused the emergence and rise of azole-resistant fungi. The fungistatic nature of FLC in combination with toxicity concerns have resulted in an increased demand for new azole antifungal agents.
Nishad Thamban Chandrika +5 more
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Introduction of Substituents on the 2-Oxo-piperazine Skeleton by [3+2] Cycloaddition and Subsequent Transformation [PDF]
, 2006 The 3,4-substituted 2-oxo-piperazines 5 - 9 are obtained by [3+2] cycloaddition from nitrone 1 and a variety of alkenes. Subsequent functionalization of the bicyclic adducts involves reductive N-O bond cleavage. A route towards libraries of immobilized 1,
Rück-Braun, Karola, Wierschem, Frank
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Investigation of piperazines as human carbonic anhydrase I, II, IV and VII activators
Journal of Enzyme Inhibition and Medicinal Chemistry, 2018 Four human (h) carbonic anhydrase isoforms (CA, EC 4.2.1.1), hCA I, II, IV, and VII, were investigated for their activation profile with piperazines belonging to various classes, such as N-aryl-, N-alkyl-, N-acyl-piperazines as well as 2,4-disubstituted ...
Andrea Angeli +4 more
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Discovery of a novel piperazine derivative, cmp2: a selective TRPC6 activator suitable for treatment of synaptic deficiency in Alzheimer’s disease hippocampal neurons [PDF]
Scientific ReportsAlzheimer disease (AD) is characterized by progressive loss of memory. Synaptic loss is now the best correlate of cognitive dysfunction in patients with Alzheimer’s disease.
Nikita Zernov +5 more
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Opportunities and challenges for direct C–H functionalization of piperazines
Beilstein Journal of Organic Chemistry, 2016 Piperazine ranks within the top three most utilized N-heterocyclic moieties in FDA-approved small-molecule pharmaceuticals. Herein we summarize the current synthetic methods available to perform C–H functionalization on piperazines in order to lend ...
Zhishi Ye, Kristen E. Gettys, Mingji Dai
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