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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Visible Light-Mediated, Diastereoselective Epimerization of Morpholines and Piperazines to More Stable Isomers. [PDF]
ACS Catal, 2022 We report a photocatalyzed epimerization of morpholines and piperazines that proceeds by reversible hydrogen atom transfer (HAT) and provides an efficient strategy for editing the stereochemical configurations of these saturated nitrogen heterocycles ...
Shen Z +4 more
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Design, Synthesis and Biological Evaluation of Novel N-Arylpiperazines Containing a 4,5-Dihydrothiazole Ring [PDF]
Pharmaceuticals, 2023 Arylpiperazines represent one of the most important classes of 5-HT1AR ligands and have attracted considerable interests for their versatile properties in chemistry and pharmacology, leading to the research of new derivatives that has been focused on the
Giorgia Andreozzi +14 more
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Alkylated Piperazines and Piperazine-Azole Hybrids as Antifungal Agents. [PDF]
Journal of Medicinal Chemistry, 2018 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 ...
Nishad Thamban Chandrika +5 more
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Development of Piperazine- and Oxazine-Linked Pyrimidines as p65 Subunit Binders of NF–κB in Human Breast Cancer Cells [PDF]
Biomedicines, 2023 Nuclear factor kappa B (NF–κB) is a potential therapeutic target in breast cancer. In the current study, a new class of oxazine– and piperazine–linked pyrimidines was developed as inhibitors of NF–κB, overcoming the complexity of the oxazine structure ...
Akshay Ravish +10 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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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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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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Harnessing unprotected deactivated amines and arylglyoxals in the Ugi reaction for the synthesis of fused complex nitrogen heterocycles [PDF]
Beilstein Journal of Organic ChemistryPiperazines and diazepines are examples of nitrogen heterocycles present in many marketed drugs highlighting their importance in the discovery of novel bioactive compounds.
Javier Gómez-Ayuso +5 more
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Determination of Piperazine [PDF]
Journal of AOAC INTERNATIONAL, 1960 Sam H Perlmutter
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