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1

Tang, Yao, Nvjiang Wu, Junyu Xu, Xiaopo Zhang, Youbin Li, and Xuesong Wang. "Metal-Free Cascade Formation of C–C and C–N Bond for the Construction of 3-Cyano-2-Pyridones with Insecticidal Properties." Molecules 29, no. 12 (2024): 2792. http://dx.doi.org/10.3390/molecules29122792.

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A straightforward and efficient methodology has been developed for the synthesis of 3-cyano-2-pyridones via the C–C and C–N bond formation processes. A total of 51 diverse 3-cyano-2-pyridone derivatives were obtained in moderate to excellent yields. This reaction featured advantages such as a metal-free process, wide functional group tolerance, simple operation, and mild conditions. A plausible mechanism for the reaction was proposed. 3-cyano-2-pyridones as ricinine analogues for insecticidal properties were evaluated, and the compound 3ci (LC50 = 2.206 mg/mL) showed the best insecticidal prop
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2

Yang, Yinghua, Lianli Sun, Shengyi Dong, et al. "Synthesis of the pyridone analogues of territrem B." Mendeleev Communications 18, no. 4 (2008): 186–87. http://dx.doi.org/10.1016/j.mencom.2008.07.004.

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3

Kaur, Ishwinder, Gopal P. Jadhav, Peter M. Fischer, and Gerlof Sebastiaan Winkler. "The Discovery of Substituted 5-(2-Hydroxybenzoyl)-2-Pyridone Analogues as Inhibitors of the Human Caf1/CNOT7 Ribonuclease." Molecules 29, no. 18 (2024): 4351. http://dx.doi.org/10.3390/molecules29184351.

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The Caf1/CNOT7 nuclease is a catalytic component of the Ccr4-Not deadenylase complex, which is a key regulator of post-transcriptional gene regulation. In addition to providing catalytic activity, Caf1/CNOT7 and its paralogue Caf1/CNOT8 also contribute a structural function by mediating interactions between the large, non-catalytic subunit CNOT1, which forms the backbone of the Ccr4-Not complex and the second nuclease subunit Ccr4 (CNOT6/CNOT6L). To facilitate investigations into the role of Caf1/CNOT7 in gene regulation, we aimed to discover and develop non-nucleoside inhibitors of the enzyme
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4

Hwang, Gil Tae, Aaron M. Leconte, and Floyd E. Romesberg. "Polymerase Recognition and Stability of Fluoro-Substituted Pyridone Nucleobase Analogues." ChemBioChem 8, no. 13 (2007): 1606–11. http://dx.doi.org/10.1002/cbic.200700308.

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5

Capps, Nigel K., Gareth M. Davies, David Loakes, Richard W. McCabe та Douglas W. Young. "Synthesis of bicyclic pyridone and dihydropyridone analogues of β-lactam antibiotics". J. Chem. Soc., Perkin Trans. 1, № 12 (1991): 3077–86. http://dx.doi.org/10.1039/p19910003077.

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6

Rubovič, Peter, Andriy Pysanenko, Jozef Lengyel, Dana Nachtigallová, and Michal Fárník. "Biomolecule Analogues 2-Hydroxypyridine and 2-Pyridone Base Pairing on Ice Nanoparticles." Journal of Physical Chemistry A 120, no. 27 (2016): 4720–30. http://dx.doi.org/10.1021/acs.jpca.5b11359.

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7

Haffner, Curt D., Caroline J. Diaz, Aaron B. Miller, et al. "Pyrrolidinyl pyridone and pyrazinone analogues as potent inhibitors of prolyl oligopeptidase (POP)." Bioorganic & Medicinal Chemistry Letters 18, no. 15 (2008): 4360–63. http://dx.doi.org/10.1016/j.bmcl.2008.06.067.

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8

Tauraitė, Daiva, Rytis Ražanas, Algirdas Mikalkėnas, Saulius Serva, and Rolandas Meškys. "Synthesis of Pyridone-based Nucleoside Analogues as Substrates or Inhibitors of DNA Polymerases." Nucleosides, Nucleotides and Nucleic Acids 35, no. 4 (2016): 163–77. http://dx.doi.org/10.1080/15257770.2015.1122197.

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9

CAPPS, N. K., G. M. DAVIES, D. LOAKES, R. W. MCCABE та D. W. YOUNG. "ChemInform Abstract: Synthesis of Bicyclic Pyridone and Dihydropyridone Analogues of β- Lactam Antibiotics." ChemInform 23, № 13 (2010): no. http://dx.doi.org/10.1002/chin.199213234.

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10

Murgatroyd, Christopher, Lisa Pirrie, Fanny Tran, Terry K. Smith, Nicholas J. Westwood, and Catherine S. Adamson. "Structure-Activity Relationships of the Human Immunodeficiency Virus Type 1 Maturation Inhibitor PF-46396." Journal of Virology 90, no. 18 (2016): 8181–97. http://dx.doi.org/10.1128/jvi.01075-16.

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ABSTRACTHIV-1 maturation inhibitors are a novel class of antiretroviral compounds that consist of two structurally distinct chemical classes: betulinic acid derivatives and the pyridone-based compound PF-46396. It is currently believed that both classes act by similar modes of action to generate aberrant noninfectious particles via inhibition of CA-SP1 cleavage during Gag proteolytic processing. In this study, we utilized a series of novel analogues with decreasing similarity to PF-46396 to determine the chemical groups within PF-46396 that contribute to antiviral activity, Gag binding, and th
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11

Gemma, Sandra, Stefania Butini, Caterina Fattorusso, et al. "A palladium-catalyzed synthetic approach to new Huperzine A analogues modified at the pyridone ring." Tetrahedron 59, no. 1 (2003): 87–93. http://dx.doi.org/10.1016/s0040-4020(02)01449-7.

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12

Becknell, Nadine C., Jacquelyn A. Lyons, Lisa D. Aimone, et al. "Synthesis and evaluation of pyridone-phenoxypropyl-R-2-methylpyrrolidine analogues as histamine H3 receptor antagonists." Bioorganic & Medicinal Chemistry Letters 21, no. 23 (2011): 7076–80. http://dx.doi.org/10.1016/j.bmcl.2011.09.091.

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13

Basheerulla, Shaik, Kaushal Tripti, and K. Agrawal Vijay. "Quantitative structure activity relationship studies on a series of 4-pyridones as antimalerial agents." Journal of Indian Chemical Society 93, Jul 2016 (2016): 871–76. https://doi.org/10.5281/zenodo.5638287.

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Department of Applied Sciences, NITTTR, Shamla Hills, Bhopal-462 002, Madhya Pradesh, India E-mail : basheerulla.81@gmail.com Department of Chemistry, Technocrats Institute of Technology and Science, Bhopal, Madhya Pradesh, India Department of Chemistry, A. P. S. University, Rewa-486 003, Madhya Pradesh, India <em>E-mail</em> : apsvka@yahoo.co.in Quantitative structure-activity relationship (QSAR) studies have been performed on a series of twenty four (24) 4-pyridone analogues as antimalarial agents. A genetic algorithm multiple linear regression (GA-MLR) analysis has shown that three-variable
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14

Ling, Lin, Chen Ling, and Hua Wu. "In vitro evaluation of the inhibitory effect of 3, 5-dichloro-2- pyridone on Mycobacterium tuberculosis H37Rv." Tropical Journal of Pharmaceutical Research 19, no. 1 (2020): 163–68. http://dx.doi.org/10.4314/tjpr.v19i1.24.

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Purpose: To investigate the anti-tuberculosis potential of twelve commercially available pyridone analogues against Mycobacterium tuberculosis H37Rv strain.Methods: Twelve commercially available pyridone-based compounds were screened against M. tuberculosis H37Rv using different susceptibility tests. The most active or lead compound was further evaluated in detail for its anti-tuberculosis (anti-TB) potential. Kill kinetics was used to determine the dynamics of its anti-TB activity in vitro.Results: Compounds d, j and k were potent against M. tuberculosis H37Rv, with minimum inhibitory concent
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15

Wang, Qiang, Xueyuan Hu, Qiulin Kuang, Dan Li, Huili Wu, and Jianyong Yuan. "A series of new polycyclic carbamoyl pyridone analogues were synthesized by using chloroacetaldehyde as a substrate." Tetrahedron 88 (May 2021): 132156. http://dx.doi.org/10.1016/j.tet.2021.132156.

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16

Sengupta, Tista, Krishnanka S. Gayen, Palash Pandit, and Dilip K. Maiti. "FeCl3⋅6H2O-Catalyzed Intermolecular-Cascade Cyclization of Acetoacetanilide: Aldehyde-Tuned Synthesis to Valuable 2-Pyridone Analogues." Chemistry - A European Journal 18, no. 7 (2012): 1905–9. http://dx.doi.org/10.1002/chem.201103354.

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17

Lin, Xiaojing, Siwen Yuan, Senhua Chen, et al. "Heterologous Expression of Ilicicolin H Biosynthetic Gene Cluster and Production of a New Potent Antifungal Reagent, Ilicicolin J." Molecules 24, no. 12 (2019): 2267. http://dx.doi.org/10.3390/molecules24122267.

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Ilicicolin H is a broad-spectrum antifungal agent targeting mitochondrial cytochrome bc1 reductase. Unfortunately, ilicicolin H shows reduced activities in vivo. Here, we report our effort on the identification of ilicicolin H biosynthetic gene cluster (BGC) by genomic sequencing a producing strain, Neonectria sp. DH2, and its heterologous production in Aspergillus nidulans. In addition, a shunt product with similar antifungal activities, ilicicolin J, was uncovered. This effort would provide a base for future combinatorial biosynthesis of ilicicolin H analogues. Bioinformatics analysis sugges
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18

Campiani, Giuseppe, Alan P. Kozikowski, Shaomeng Wang, et al. "Synthesis and anticholinesterase activity of huperzine A analogues containing phenol and catechol replacements for the pyridone ring." Bioorganic & Medicinal Chemistry Letters 8, no. 11 (1998): 1413–18. http://dx.doi.org/10.1016/s0960-894x(98)00229-7.

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19

Müller, Andreas, and Samuel Leutwyler. "Nucleobase Pair Analogues 2-Pyridone·Uracil, 2-Pyridone·Thymine, and 2-Pyridone·5-Fluorouracil: Hydrogen-Bond Strengths and Intermolecular Vibrations." Journal of Physical Chemistry A 108, no. 29 (2004): 6156–64. http://dx.doi.org/10.1021/jp049033h.

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20

Singh, Neelu, Basheerulla Shaik, Neeraj Agrawal, Anita K, Vijay K. Agrawal, and Satya P. Gupta. "QSAR and Molecular Modeling Studies on a Series of Indole-based Pyridone Analogues as HCV NS5B Polymerase Inhibitors." Letters in Drug Design & Discovery 13, no. 8 (2016): 757–70. http://dx.doi.org/10.2174/1570180813666160815122359.

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21

Sengupta, Tista, Krishnanka S. Gayen, Palash Pandit, and Dilip K. Maiti. "ChemInform Abstract: FeCl3·6H2O-Catalyzed Intermolecular-Cascade Cyclization of Acetoacetanilide: Aldehyde-Tuned Synthesis to Valuable 2-Pyridone Analogues." ChemInform 43, no. 26 (2012): no. http://dx.doi.org/10.1002/chin.201226153.

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22

CAMPIANI, G., A. P. KOZIKOWSKI, S. WANG, et al. "ChemInform Abstract: Synthesis and Anticholinesterase Activity of Huperzine A Analogues Containing Phenol and Catechol Replacements for the Pyridone Ring." ChemInform 29, no. 42 (2010): no. http://dx.doi.org/10.1002/chin.199842209.

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23

Pazderski, Leszek, and Pavel A. Abramov. "Au(III) Cyclometallated Compounds with 2-Arylpyridines and Their Derivatives or Analogues: 34 Years (1989–2022) of NMR and Single Crystal X-ray Studies." Inorganics 11, no. 3 (2023): 100. http://dx.doi.org/10.3390/inorganics11030100.

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A review paper on Au(III) cyclometallated compounds with 2-arylpyridines (2-phenylpyridine, 2-benzylpyridine, 2-benzoylpyridine, 2-phenoxypyridine, 2-phenylsulfanylpyridine, 2-anilinopyridine, 2-(naphth-2-yl)pyridine, 2-(9,9-dialkylfluoren-2-yl)pyridines, 2-(dibenzofuran-4-yl)pyridine, and their derivatives) and their analogues (2-arylquinolines, 1- and 3-arylisoquinolines, 7,8-benzoquinoline), with 113 references. A total of 554 species, containing κ2-N(1),C(6′)*-Au(III), or analogous moiety (i.e., chelated by nitrogen of the pyridine-like ring and the deprotonated ortho- carbon of the phenyl
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24

Denisov, Gleb L., and Yulia V. Nelyubina. "New Co-Crystals/Salts of Gallic Acid and Substituted Pyridines: An Effect of Ortho-Substituents on the Formation of an Acid–Pyridine Heterosynthon." Crystals 12, no. 4 (2022): 497. http://dx.doi.org/10.3390/cryst12040497.

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Co-crystallization of gallic acid with pyridines and their polyaromatic analogue, quinoline, ortho-substituted by various proton-donating groups able to form hydrogen bonds, produced the only reported co-crystal of gallic acid with an ortho-substituted pyridine, 2-hydroxypyridine, as its preferred pyridone-2 tautomer, and four new crystalline products of gallic acid. These co-crystals, or gallate salts depending on the choice of the pyridine-containing compound, as predicted by the pKa rule, were identified by X-ray diffraction to feature the popular acid–pyridine heterosynthon found in most o
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25

Schmitt, Martine, Jean-Jacques Bourguignon, Gordon B. Barlin, and Les P. Davies. "Imidazo[1,2-b]pyridazines. XXIII Some 5-Deaza Analogues. Syntheses of Some 2-Aryl-6-(chloro, methoxy or unsubstituted)-3- (variously substituted)imidazo[1,2-a]pyridines and Their Affinity for Central and Mitochondrial Benzodiazepine Receptor." Australian Journal of Chemistry 50, no. 7 (1997): 719. http://dx.doi.org/10.1071/c97004.

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The syntheses of ethyl {2′-aryl-6′-(chloro, methoxy and unsubstituted)imidazo[1,2-a]pyridin-3′-yl}-2- (acylamino, acetoxy and hydroxy)acetates, 3-benzamidomethyl-2-benzoyl-6-(chloro and methoxy)imidazo-[1,2-a]pyridines, 3-amino-6-chloro-2-phenylimidazo[1,2-a]pyridine and ethyl 2-(2′-phenylimidazo[1,2-a]pyridin-3′-yl)acetate are reported. The ability of these compounds to displace [3H]diazepam from central and mitochondrial (peripheral-type) benzodiazepine receptors has been examined. Ethyl 2-benzamido-2-{6′-chloro-2′-(4′′-chlorophenyl)imidazo[1,2-a]pyridin-3′-yl} acetate (21) was selective for
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26

Karis, N. David, Wendy A. Loughlin, and Ian D. Jenkins. "A facile and efficient method for the synthesis of novel pyridone analogues by aminolysis of an ester under solvent-free conditions." Tetrahedron 63, no. 50 (2007): 12303–9. http://dx.doi.org/10.1016/j.tet.2007.09.068.

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27

Hakobyan, Robert M., Havhannes V. Adunts, Havhannes S. Attaryan, et al. "NEW C1 AND N5 DERIVATIVES OF CERPEGINE. SYNTHESIS AND ANTIBACTERIAL ACTIVITY STUDY." ChemChemTech 68, no. 7 (2025): 35–47. https://doi.org/10.6060/ivkkt.20256807.7224.

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This study explores the bioactive properties of synthetic compounds containing γ-lactone and 2-pyridone ring systems, which exhibit a broad spectrum of pharmacological activities. These compounds are structural analogues of the alkaloid serpegin, originally isolated from Ceropegia juncea, a plant known in traditional Indian medicine for its therapeutic effects. Serpegin has been reported to possess sedative, anti-inflammatory, analgesic, and anti-ulcer properties, making its synthetic analogues attractive candidates for the development of novel therapeutic agents. Among the synthetic derivativ
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28

Bartulewicz, D., K. Bielawski, A. Markowska, K. Zwierz, A. Pućkowska, and A. Rózański. "Synthetic analogues of netropsin and distamycin--synthesis of a new pyridine and carbocyclic analogues of the pyrrolecarboxamide antitumour antibiotics." Acta Biochimica Polonica 45, no. 1 (1998): 41–57. http://dx.doi.org/10.18388/abp.1998_4317.

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A new series of pyridine-containing analogues III-XXII of distamycin A and netrop sin was investigated by the molecular mechanics technique and molecular modelling. A pyridine analogue of netropsin (VII) is described, the first compound based on molecular studies, and two carbocyclic analogues of distamycin A with an N-terminal chloro- or bromoacetyl group (VIa, VIIa) were synthesized, as well as carbocyclic analogues of netropsin (VIIIb, Xb), potential carriers of alkylating elements. The potential use of VIa, VII, VIIa, VIIIb and Xb as carriers to place into the minor groove of DNA chemical
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29

Elgemee, Galal H., Hosny A. Ali, Ahmed H. Elghandour, and Ghada W. Abd Elaziz. "SYNTHESIS OF NOVEL DERIVATIVES OF 4-METHYLTHIO-N-ARYL-2-PYRIDONE AND DEAZAPURINE ANALOGUES: THE REACTION OF KETENE DITHIOACETALS WITH SUBSTITUTED ACETANILIDES." Phosphorus, Sulfur, and Silicon and the Related Elements 164, no. 1 (2000): 189–97. http://dx.doi.org/10.1080/10426500008045245.

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30

Shyam, Mousumi, Abhimanyu Dev, Barij Nayan Sinha, and Venkatesan Jayaprakash. "Scaffold Based Search on the Desferithiocin Archetype." Mini-Reviews in Medicinal Chemistry 19, no. 19 (2019): 1564–76. http://dx.doi.org/10.2174/1389557519666190301151151.

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:Iron overload disorder and diseases where iron mismanagement plays a crucial role require orally available iron chelators with favourable pharmacokinetic and toxicity profile. Desferrithiocin (DFT), a tridentate and orally available iron chelator has a favourable pharmacokinetic profile but its use has been clinically restricted due to its nephrotoxic potential. The chemical architecture of the DFT has been naturally well optimized for better iron chelation and iron clearance from human biological system. Equally they are also responsible for its toxicity. Hence, subsequent research has been
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31

Mo, Dong-Liang, Xiao-Hua Li, Ai-Hui Ye, and Cui Liang. "Substituent Effects of 2-Pyridones on Selective O-Arylation with Diaryliodonium Salts: Synthesis of 2-Aryloxypyridines under Transition­-Metal-Free Conditions." Synthesis 50, no. 08 (2018): 1699–710. http://dx.doi.org/10.1055/s-0036-1591884.

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An efficient transition-metal-free strategy to synthesize 2-aryloxypyridine derivatives has been developed by a selective O-arylation of 2-pyridones with diaryliodonium salts. The reaction was compatible with a series of functional groups for 2-pyridones and diaryliodonium salts such as halides, nitro, cyano, and ester groups. The substituents at the C6-position of 2-pyridones favored O-arylation products because of steric hindrance. The reaction was easily performed on a gram-scale and 6-chloro-2-pyridone was a good precursor to access various unsubstituted 2-aryloxypyridines by dehalogenatio
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32

BEHOLZ, L. G., P. BENOVSKY, D. L. WARD, N. S. BARTA та J. R. STILLE. "ChemInform Abstract: Formation of Dihydropyridone- and Pyridone-Based Peptide Analogues Through Aza-Annulation of β-Enamino Ester and Amide Substrates with α-Amido Acrylate Derivatives." ChemInform 28, № 27 (2010): no. http://dx.doi.org/10.1002/chin.199727145.

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33

Hwang, Jimin, Natalie Strange, Matthew J. A. Phillips, et al. "Optimization of peptide-based inhibitors targeting the HtrA serine protease in Chlamydia: Design, synthesis and biological evaluation of pyridone-based and N-Capping group-modified analogues." European Journal of Medicinal Chemistry 224 (November 2021): 113692. http://dx.doi.org/10.1016/j.ejmech.2021.113692.

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34

Czarnocki, Zbigniew, and Piotr Pomarański. "Arylpyridines: A Review from Selective Synthesis to Atropisomerism." Synthesis 51, no. 03 (2018): 587–611. http://dx.doi.org/10.1055/s-0037-1611365.

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Multiply arylated heterocycles are interesting structures with highly useful functions and fascinating optoelectronic and biological properties. Pyridines are an important class of compounds, playing a role in various fields of chemistry. When the pyridine ring is connected to other aromatic systems, novel stereochemical outcomes may arise. This work summarizes different methodologies applied for the synthesis of substituted arylpyridine derivatives and summarizes stereochemical phenomena resulting from atropisomerism present in certain arylated pyridines.1 Introduction2 Arylpyridines Containi
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35

Semple, Graeme, Britt-Marie Andersson, Vijay Chhajlani, et al. "Synthesis and Biological activity of kappa opioid receptor agonists. Part 2: Preparation of 3-aryl-2-pyridone analogues generated by solution- and solid-phase parallel synthesis methods." Bioorganic & Medicinal Chemistry Letters 13, no. 6 (2003): 1141–45. http://dx.doi.org/10.1016/s0960-894x(03)00033-7.

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36

Watanabe, Tatsuya, Minami Odagi, Kota Furukori та Kazuo Nagasawa. "Asymmetric α-Hydroxylation of a Lactone with Vinylogous Pyridone by Using a Guanidine-Urea Bifunctional Organocatalyst: Catalytic Enantioselective Synthesis of a Key Intermediate for (20S)-Camptothecin Analogues". Chemistry - A European Journal 20, № 2 (2013): 591–97. http://dx.doi.org/10.1002/chem.201303633.

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37

Shilin, S., Z. Voitenko, and M. Nechai. "SYNTHETIC PYRIDINE SUBSTITUTED AMINO ACIDS AND THEIR DERIVATIVES." Bulletin of Taras Shevchenko National University of Kyiv. Chemistry, no. 1(56) (2019): 22–25. http://dx.doi.org/10.17721/1728-2209.2019.1(56).5.

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This paper reports on the synthesis of new derivatives of ε-aminocaproic and γ-aminobutyric acid modified with a pyridin-2-yl substituent at the ω-position of the main chain. The hemostatic activity of both ε-aminocaproic acid itself and its various synthetic analogues is widely known. Likewise, numerous γ-aminobutyric acid derivatives are strong neurotransmitters extensively used in the treatment of the nervous system disorders. No less popular are biologically active substances containing a pyridine or piperidine fragment; among which there are antibiotics, antimalarial, anti-sclerotic and a
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38

Sim, Jaeuk, Srinu Lanka, Jeong-Woong Jo та ін. "Inhibitory Effect of Chlorogenic Acid Analogues Comprising Pyridine and Pyrimidine on α-MSH-Stimulated Melanogenesis and Stability of Acyl Analogues in Methanol". Pharmaceuticals 14, № 11 (2021): 1176. http://dx.doi.org/10.3390/ph14111176.

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In continuation of studies for α-MSH stimulated melanogenesis inhibitors, we have evaluated the design, synthesis, and activity of a new series of chlorogenic acid (CGA) analogues comprising pyridine, pyrimidine, and diacyl derivatives. Among nineteen synthesized compounds, most of them (fifteen) exhibited better inhibitions of melanin formation in B16 melanoma cells. The results illustrated that a pyridine analogue 6f and a diacyl derivative 13a of CGA showed superior inhibition profiles (IC50: 2.5 ± 0.7 μM and 1.1 ± 0.1 μM, respectively) of α-MSH activities than positive controls, kojic acid
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39

Dahikar, Girish D., and Rajendra O. Ganjiwale. "Synthesis, Spectral Characterization, in silico Molecular Docking and Pharmacological Screening of Some Quinazoline Analogues as Anticonvulsants." Asian Journal of Chemistry 37, no. 6 (2025): 1415–20. https://doi.org/10.14233/ajchem.2025.33816.

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A new analogues of 2-methyl-3-(6-substituted-benzothiazol-2-yl)-3H-quinazolin-4-one [Dm1-Dm5] and their 6-bromo analogues [Dm6-Dm10], similarly a new analogues of 2-methyl-3-(pyridin-4-yl-formamide)-3H-quinazolin-4-one [Em1] and its 6-bromo analogue [Em2] were synthesized and characterized by melting point, elemental and spectral [FTIR, (1H and 13C) NMR and MS] methods. The anticonvulsant activity of selected analogues was assessed against maximal electroshock (MES) induced convulsions model in albino mice. The selected analogues were injected intraperitoneally at dose 20 mg/kg body weight and
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40

Watanabe, Tatsuya, Minami Odagi, Kota Furukori та Kazuo Nagasawa. "ChemInform Abstract: Asymmetric α-Hydroxylation of a Lactone with Vinylogous Pyridone by Using a Guanidine-Urea Bifunctional Organocatalyst: Catalytic Enantioselective Synthesis of a Key Intermediate for (20S)-Camptothecin Analogues." ChemInform 45, № 23 (2014): no. http://dx.doi.org/10.1002/chin.201423036.

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41

Chavchich, Marina, Geoffrey W. Birrell, Arba L. Ager, et al. "Lead Selection of a New Aminomethylphenol, JPC-3210, for Malaria Treatment and Prevention." Antimicrobial Agents and Chemotherapy 60, no. 5 (2016): 3115–18. http://dx.doi.org/10.1128/aac.03066-15.

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ABSTRACTStructure-activity relationship studies of trifluoromethyl-substituted pyridine and pyrimidine analogues of 2-aminomethylphenols (JPC-2997, JPC-3186, and JPC-3210) were conducted for preclinical development for malaria treatment and/or prevention. Of these compounds, JPC-3210 [4-(tert-butyl)-2-((tert-butylamino)methyl)-6-(5-fluoro-6-(trifluoromethyl)pyridin-3-yl)phenol] was selected as the lead compound due to superiorin vitroantimalarial activity against multidrug-resistantPlasmodium falciparumlines, lowerin vitrocytotoxicity in mammalian cell lines, longer plasma elimination half-lif
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42

Zhang, Guoqi. "4-vinylpyridine derivatives: Protonation, methylation and silver(I) coordination chemistry." Journal of Chemical Research 45, no. 7-8 (2021): 687–93. http://dx.doi.org/10.1177/1747519821989659.

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( E)-4-[2-(Pyridin-4-yl)vinyl]benzaldehyde, containing both a 4-vinylpyridine and an aldehyde functionality, is utilized to develop new, highly conjugated chalcone compounds and a bis-Schiff base azine compound. The chalcone-containing compounds are further explored for their protonation, methylation and silver(I) coordination chemistry using the pyridine moiety. In parallel, a cyano-containing analogue, ( E)-4-[2-(pyridin-4-yl)vinyl]benzonitrile is also synthesized and studied for its silver(I) coordination chemistry. These new compounds are fully characterized by mass spectrometry, elemental
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43

Larkina, M. S., E. V. Podrezova, O. D. Bragina, et al. "Development of a method for preparing octreotide derivative for diagnosis of neuroendocrine tumors." Bulletin of Siberian Medicine 18, no. 3 (2019): 72–80. http://dx.doi.org/10.20538/1682-0363-2019-3-72-80.

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Currently the development of technologies for labeling somatostatin with technetium-99m for diagnosing radionuclide neuroendocrine tumors is under way. Somatostatin analogues are binded with technetium99m only by the preliminary addition of a chelating agent. Therefore, it is important to develop a method for preparation of an octreotide derivative by modifying octreotide with precursors: ligands with high chelating ability for its tight binding with technetium-99m. ω-Bis(pyridin-2-ylmethyl)amino)aliphatic acids can be used successfully as such precursors.The purpose of the study was to develo
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44

Wu, Dan, Na Qin, Qi-Kui Liu, Jian-Ping Ma, and Yu-Bin Dong. "The structures of three Hg2X4L2macrocycles {X= Cl, Br and I, andL= 1,2-bis[4-(pyridin-3-yl)phenoxy]ethane} assembled from ether-bridged dipyridyl ligands." Acta Crystallographica Section C Crystal Structure Communications 68, no. 6 (2012): m156—m160. http://dx.doi.org/10.1107/s0108270112019075.

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The new ether-bridged dipyridyl ligand 1,2-bis[4-(pyridin-3-yl)phenoxy]ethane (L) has been used to synthesize three isostructural centrosymmetric binuclear HgIImacrocycles, namely bis{μ-1,2-bis[4-(pyridin-3-yl)phenoxy]ethane-κ2N:N′}bis[dichloridomercury(II)], [Hg2Cl4(C24H20N2O2)2], and the bromido, [Hg2Br4(C24H20N2O2)2], and iodido, [Hg2I4(C24H20N2O2)2], analogues. The Hg atoms adopt a highly distorted tetrahedral coordination environment consisting of two halides and two pyridineN-donor atoms from two bridging ligands. In the solid state, the macrocycles form two-dimensional sheets in thebcpl
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45

Niu, Xiang-Long, Lin Wei, Jian-Cheng Liu, et al. "Syntheses and structures of three macrocyclic supramolecular complexes and one ZnII-containing coordination polymer generated from a semi-rigid multidentate N-containing ligand." Acta Crystallographica Section C Structural Chemistry 77, no. 1 (2021): 29–39. http://dx.doi.org/10.1107/s2053229620016083.

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Semirigid organic ligands can adopt different conformations to construct coordination polymers with more diverse structures when compared to those constructed from rigid ligands. A new asymmetric semirigid organic ligand, 4-{2-[(pyridin-3-yl)methyl]-2H-tetrazol-5-yl}pyridine (L), has been prepared and used to synthesize three bimetallic macrocyclic complexes and one coordination polymer, namely, bis(μ-4-{2-[(pyridin-3-yl)methyl]-2H-tetrazol-5-yl}pyridine)bis[dichloridozinc(II)] dichloromethane disolvate, [Zn2Cl4(C12H10N6)2]·2CH2Cl2, (I), the analogous chloroform monosolvate, [Zn2Cl4(C12H10N6)2
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46

Pazderski, Leszek, and Pavel A. Abramov. "Pd(II), Pd(III) and Pd(IV) Cyclometallated Compounds with 2-Arylpyridines and Their Derivatives or Analogues: 44 Years (1980–2023) of NMR and Single Crystal X-ray Studies." Crystals 13, no. 10 (2023): 1482. http://dx.doi.org/10.3390/cryst13101482.

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In this paper, a review on Pd(II), Pd(III), and Pd(IV) cyclometallated compounds with 2-arylpyridines (2-phenylpyridine, 2-benzylpyridine, 2-benzoylpyridine, 2-phenoxypyridine, 2-phenylsulfanylpyridine, 2-anilinopyridine, 2-(naphth-1-yl)pyridine, 2-(naphth-2-yl)pyridine, and their derivatives) and their analogues (2-phenylquinoline and 7,8-benzoquinoline) with 174 references is presented. A total of 672 species, containing κ2-N(1),C(6′)*-palladium (Pd(II), Pd(III), Pd(IV)) or analogous moiety (i.e., chelated by nitrogen of the pyridine-like ring and the deprotonated ortho-carbon of the phenyl-
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47

Rotter, Markus, Matthias Mastalir, Mathias Glatz, Berthold Stöger, and Karl Kirchner. "Crystal structure of the tetrahydrofuran disolvate of a 94:6 solid solution of [N2,N6-bis(di-tert-butylphosphanyl)pyridine-2,6-diamine]dibromidomanganese(II) and its monophosphine oxide analogue." Acta Crystallographica Section E Crystallographic Communications 73, no. 9 (2017): 1308–11. http://dx.doi.org/10.1107/s2056989017011276.

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The MnBr2complex ofN2,N6-bis(di-tert-butylphosphanyl)pyridine-2,6-diamine (1·MnBr2) co-crystallizes with 5.69% of the monophosphine oxide analogue (1O·MnBr2) and two tetrahydrofuran (THF) molecules, namely [N2,N6-bis(di-tert-butylphosphanyl)pyridine-2,6-diamine]dibromidomanganese(II)–[bis(di-tert-butylphosphanyl)({6-[(di-tert-butylphosphanyl)amino]pyridin-2-yl}amino)phosphine oxide]dibromidomanganese(II)–tetrahydrofuran (0.94/0.06/2), [MnBr2(C21H41N3P2)]0.94[MnBr2(C21H41N3OP2)]0.06·2C4H8O. The1·MnBr2and1O·MnBr2complexes are occupationally disordered about general positions. Both complexes feat
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48

Norman, Rebecca E., Michael V. Perkins, Andris J. Liepa, and Craig L. Francis. "N,N-Dialkyl-N′-Chlorosulfonyl Chloroformamidines in Heterocyclic Synthesis. Part X. The First Pyrazolo[1,5-b][1,2,4,6]thiatriazine Derivatives and their Unusual Reactions with Acylating Agents." Australian Journal of Chemistry 66, no. 11 (2013): 1323. http://dx.doi.org/10.1071/ch13282.

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N,N-dialkyl-N′-chlorosulfonyl chloroformamidines 1 underwent a regioselective reaction with 3-aminopyrazoles 2 to produce pyrazolo[1,5-b][1,2,4,6]thiatriazines 3, representatives of a new ring system. Attempted N-acylation of compounds 3 with acetic anhydride (or chloride) and benzoyl chloride in pyridine, only afforded 5-(pyridin-4-yl)-pyrazolo[1,5-b][1,2,4,6]thiatriazine derivatives 11. The analogous reaction with pyridazine led to the corresponding pyridazin-4-yl derivative.
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49

Buchstaller, H. P., C. D. Siebert, R. H. Lyssy та ін. "Thieno[2,3-b)pyridinones as Antagonists on the Glycine Site of the N-methyl-ᴅ-aspartate Receptor - Binding Studies, Molecular Modeling and structure-Activity-Relationships". Scientia Pharmaceutica 68, № 1 (2000): 1–14. http://dx.doi.org/10.3797/scipharm.aut-00-01.

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Within the frame of the synthesis of glycine antagonists, a series of novel thieno[2,3- b]pyridinones with substituted phenyl residues in position 5 were synthesised to investigate the importance of the torsion angle between the pyridinone skeleton and the phenyl ring for binding affinity. The parent compound, 4-hydroxy-5-phenylthieno[2,3-b]pyridine-6(7H)-one, and its thienyl analogue, exhibited highest potencies, whereas compounds with ortho-substituted aryl moieties in position 5 showed decreased activities. This seems to be due to unfavourable steric interactions and increased torsion angle
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50

Bullen, Neil J., and John D. Kennedy. "Polyhedral Monocarbaborane Chemistry. Functionality and Isomerism: Reactions of the [6-Ph-nido-6-CB9H11]- Anion with Aminopyridines NC5H4NH2 to Yield Neutral arachno and closo Ten-Vertex Monocarbaborane Derivatives." Collection of Czechoslovak Chemical Communications 70, no. 11 (2005): 1873–90. http://dx.doi.org/10.1135/cccc20051873.

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Reaction of NC5H4-2-NH2 with the [6-Ph-nido-6-CB9H11]- anion (1) in the presence of hydrated FeCl3 gives [6-Ph-9-(NC5H4-2-NH2)-arachno-6-CB9H12] (4) and thence [1-Ph-2-(NC5H4-2-NH2)-closo-1-CB9H8] (5), in which the pyridine substituent is on a boron atom α to the cluster carbon atom. This behaviour contrasts to the reactions of organyl-substituted pyridines NC5H4R to yield neutral 9-pyridine arachno species [6-Ph-9-(NC5H4R)-arachno-6-CB9H12] and thence neutral 6-pyridine closo species [1-Ph-6-(NC5H4R)-closo-1-CB9H8], in which the pyridine substituent is on a boron atom β to the cluster carbon
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