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Journal articles on the topic 'Quinolone derivative'

Author: Grafiati

Published: 4 June 2025

Last updated: 1 August 2025

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1

Shoji, Taku, Mutsumi Takeuchi, Mayumi Uda, et al. "Synthesis of Azuleno[2,1-b]quinolones and Quinolines via Brønsted Acid-Catalyzed Cyclization of 2-Arylaminoazulenes." Molecules 28, no. 15 (2023): 5785. http://dx.doi.org/10.3390/molecules28155785.

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Quinolone and quinoline derivatives are frequently found as substructures in pharmaceutically active compounds. In this paper, we describe a procedure for the synthesis of azuleno[2,1-b]quinolones and quinolines from 2-arylaminoazulene derivatives, which are readily prepared via the aromatic nucleophilic substitution reaction of a 2-chloroazulene derivative with several arylamines. The synthesis of azuleno[2,1-b]quinolones was established by the Brønsted acid-catalyzed intramolecular cyclization of 2-arylaminoazulene derivatives bearing two ester groups at the five-membered ring. The halogenat

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2

Valencia, Jhesua, Oriel A. Sánchez-Velasco, Jorge Saavedra-Olavarría, Patricio Hermosilla-Ibáñez, Edwin G. Pérez, and Daniel Insuasty. "N-Arylation of 3-Formylquinolin-2(1H)-ones Using Copper(II)-Catalyzed Chan–Lam Coupling." Molecules 27, no. 23 (2022): 8345. http://dx.doi.org/10.3390/molecules27238345.

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3-formyl-2-quinolones have attracted the scientific community’s attention because they are used as versatile building blocks in the synthesis of more complex compounds showing different and attractive biological activities. Using copper-catalyzed Chan–Lam coupling, we synthesized 32 new N-aryl-3-formyl-2-quinolone derivatives at 80 °C, in air and using inexpensive phenylboronic acids as arylating agents. 3-formyl-2-quinolones and substituted 3-formyl-2-quinolones can act as substrates, and among the products, the p-methyl derivative 9a was used as a substrate to obtain different derivatives su

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3

Yadav, Pradeep, and Y. C. Joshi. "Synthesis and Spectral Study of Novel Norfloxacin Derivatives." E-Journal of Chemistry 5, s2 (2008): 1154–58. http://dx.doi.org/10.1155/2008/357073.

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Reaction of [1-ethyl-6-fluoro-1,4-dihydro-4-oxo-7-(1-piperazinyl)-quinolone-3-carboxylic acid (norfloxacin) with thiazole / benzothiazole diazonium chloride to get new piperazine substituted norfloxacin derivative. These norfloxacin derivatives were further condensed with variousβ-diketone to get novel acid derivatives of 1-Ethyl-6-fluoro-4-oxo-7- [4 (thiazol-2-yldiazenyl)-piperzin-1-yl]-1,4-dihydro-quinoline-3-carboxylic acid (6a-e) and 7-(4-(benzo[d]thiazol-2-yldiazenyl)piperazin-1-yl)-1-ethyl-6-fluoro-4-oxo-1, 4-dihydroquinoline-3-carboxylic acid (6 f-j). Structures of these compounds were

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4

Morteza, Shiri, Nejatinezhad-Arani Atefeh, and Faghihi Zeinab. "Synthesis of Novel Quinoline-substituted 1,4-dihydropyridine Derivatives via Hantzsch Reaction in Aqueous Medium: Potential Bioactive Compounds." Journal of Heterocyclic Chemistry 54, no. 1 (2015): 131–36. https://doi.org/10.1002/jhet.2553.

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The synthesis of a novel series of substituted 1,4-dihydropyridines was achieved in aqueous media by base-catalyzed three-component Hantzsch reaction of 2chloroquinoline-3-carbaldehydes, ammonium acetate, and alkyl acteoacetate in good to high yields. Important advantages of this method are easy access to a library of novel quinoline and quinolone derivatives, green reaction conditions with water as solvent, and ease of purification.

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5

A.AlOmari, Nohad, Adnan O. Omar, and Iklas M. Taher. "Preliminary Cytotoxic Study of Some Novel Furo-2-quinolone Compounds." Iraqi Journal of Pharmaceutical Sciences ( P-ISSN: 1683 - 3597 , E-ISSN : 2521 - 3512) 18, Suppl. (2017): 32–38. http://dx.doi.org/10.31351/vol18isssuppl.pp32-38.

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In this research, new series of Furo-2-quinolone [FQ] compounds have been synthesized. These novel [FQ] compounds were prepared from coumarin derivatives (Furocoumarins: psoralen and isopsoralen).Identifications of these FQ compounds were performed by using infrared spectrum (I.R), Ultraviolet spectrum (U.V) and Nuclear Magnetic Resonance spectrum (H1-NMR) besides some physical data. The cytotoxic screening involves ;using HEP-2 cell line which gave differential responses against tested compounds : 4,6 Dimethyl furo[2, 3-g] coumarin (C1), 1-(2`, 4`, Dimethoxy benzylideneimino)-2,6-dimethyl Fur

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6

Rogerio, Kamilla Rodrigues, Cedric Stephan Graebin, Luiza Helena Pinto Domingues, et al. "Novel Quinolinyl-pyrrolo[3,4-d]pyrimidine-2,5-dione Derivatives Against Chloroquine-resistant Plasmodium falciparum." Current Topics in Medicinal Chemistry 20, no. 2 (2020): 99–110. http://dx.doi.org/10.2174/1568026619666191019100711.

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Introduction: In this work DHPMs were combined with the quinoline nucleus to obtain new quinolinyl-pyrrolo[3,4-d]pyrimidine-2,5-dione compounds with improved antiplasmodial activity as well as decreased cytotoxicity. Nineteen quinolinyl-pyrrolo[3,4-d]pyrimidine-2,5-dione derivatives connected by a linker group to quinolone ring moieties with different substituents were synthesized and assayed against P. falciparum. Materials and Methods: Nineteen quinolinyl-pyrrolo[3,4-d]pyrimidine-2,5-dione derivatives connected by a linker group to quinoline ring moieties with different substituents were syn

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7

Bonyad, Ali Moin. "Synthesis of Chalcones from Acetone and tetrazole and 2-acetyl naphthalene Assisted by Microwave." Engineering and Technology Quarterly Reviews 3, no. 1 (2020): 16–22. https://doi.org/10.5281/zenodo.3686827.

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In the present study, we understood the total synthesis one chalcone derivative via Claisen-Schmidt condensation of the respective aldehydes and ketones using Microwave assisted irradiation method. In the microwave environment, chemical reactions usually proceed faster and give higher yields with fewer by- products. In the synthesis, a common aldehyde namely tetrazolo {1, 5-a} quinoline-4-carbaldehyde was used while the ketones used were respectively acetone, 2- acetyl Naphthalene. The Chalcone synthesised from Tetrazolo {1, 5-a} quinolone-4-carbaldehyde and acetone was 4-(tetrazolo {1, 5-a} q

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8

Chokkar, Nisha, Sourav Kalra, Monika Chauhan, and Raj Kumar. "A Review on Quinoline Derived Scaffolds as Anti-HIV Agents." Mini-Reviews in Medicinal Chemistry 19, no. 6 (2019): 510–26. http://dx.doi.org/10.2174/1389557518666181018163448.

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After restricting the proliferation of CD4+T cells, Human Immunodeficiency Virus (HIV), infection persists at a very fast rate causing Acquired Immunodeficiency Syndrome (AIDS). This demands the vigorous need of suitable anti-HIV agents, as existing medicines do not provide a complete cure and exhibit drawbacks like toxicities, drug resistance, side-effects, etc. Even the introduction of Highly Active Antiretroviral Therapy (HAART) failed to combat HIV/AIDS completely. The major breakthrough in anti-HIV discovery was marked with the discovery of raltegravir in 2007, the first integrase (IN) in

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9

Mohamed, Heba A. E., and Hossa F. Al-Shareef. "Design, Synthesis, Anti-Proliferative Evaluation and Cell Cycle Analysis of Hybrid 2-Quinolones." Anti-Cancer Agents in Medicinal Chemistry 19, no. 9 (2019): 1132–40. http://dx.doi.org/10.2174/1871520619666190319142934.

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Background: Quinolones are a significant group of nitrogen heterocyclic compounds that exist in therapeutic agents, alkaloids, and synthetic small molecules that have important biological activities. A wide range of quinolones have been used as antituberculosis, antibacterial, anti-malarial, antifungal, anticonvulsant, anticancer agents and urease inhibitors. Methods: Ethyl 3,3-disubstituted-2-cyano propionates containing hybride quinolones derivatives were synthesized by the reaction of 1-amino-7-hydroxy-4-methylquinolin-2(1H)-one and its dibromo derivative with α, β-unsaturated carbonyl in e

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10

Malik, Muhammad, Kevin R. Marks, Heidi A. Schwanz, Nadezhda German, Karl Drlica, and Robert J. Kerns. "Effect of N-1/C-8 Ring Fusion and C-7 Ring Structure on Fluoroquinolone Lethality." Antimicrobial Agents and Chemotherapy 54, no. 12 (2010): 5214–21. http://dx.doi.org/10.1128/aac.01054-10.

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ABSTRACT Quinolones rapidly kill bacteria by two mechanisms, one that requires protein synthesis and one that does not. The latter, which is measured as lethal action in the presence of the protein synthesis inhibitor chloramphenicol, is enhanced by N-1 cyclopropyl and C-8 methoxy substituents, as seen with the highly lethal compound PD161144. In some compounds, such as levofloxacin, the N-1 and C-8 substituents are fused. To assess the effect of ring fusion on killing, structural derivatives of levofloxacin and PD161144 differing at C-7 were synthesized and examined with Escherichia coli. A f

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11

Saalim, Muhammad, Jessica Villegas-Moreno, and Benjamin R. Clark. "Bacterial Alkyl-4-quinolones: Discovery, Structural Diversity and Biological Properties." Molecules 25, no. 23 (2020): 5689. http://dx.doi.org/10.3390/molecules25235689.

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The alkyl-4-quinolones (AQs) are a class of metabolites produced primarily by members of the Pseudomonas and Burkholderia genera, consisting of a 4-quinolone core substituted by a range of pendant groups, most commonly at the C-2 position. The history of this class of compounds dates back to the 1940s, when a range of alkylquinolones with notable antibiotic properties were first isolated from Pseudomonas aeruginosa. More recently, it was discovered that an alkylquinolone derivative, the Pseudomonas Quinolone Signal (PQS) plays a key role in bacterial communication and quorum sensing in Pseudom

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12

M., B. DESHMUKH, and A. SHELAR M. "Synthesis of Some New N1-Substituted-6-methyl-4-phenylquinolin-2(1H)-ones." Journal of Indian Chemical Society Vol. 75, Sep 1998 (1998): 529–31. https://doi.org/10.5281/zenodo.5925724.

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Department of Chemistry, Shivaji University, Kolhapur-416 004 <em>Manuscript received 16 October 1997, revised 28 April 1998, accepted 6 May 1998</em> Quinolone (1) when <em>N</em>-alkylated with 2-chloropropionate in the presence of potassium carbonate gives 1-methoxycarbonylethy1-6- methy1-4-phenylquinolin-2(1<em>H</em>)-one (2) which on treatment with hydrazine hydrate yields 1-hydrazidoethy1-6-dimethyl-4-phenylquinolin-2(1<em>H</em>)-one (3). Compound 3 reacts with various aldehydes to form arylidene derivatives (4). Cycloaddition of 4 with mercaptoacetic acid gives thiazolidinon

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13

Kania, Agnieszka, Waldemar Tejchman, Anna M. Pawlak, et al. "Preliminary Studies of Antimicrobial Activity of New Synthesized Hybrids of 2-Thiohydantoin and 2-Quinolone Derivatives Activated with Blue Light." Molecules 27, no. 3 (2022): 1069. http://dx.doi.org/10.3390/molecules27031069.

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Thiohydantoin and quinolone derivatives have attracted researchers’ attention because of a broad spectrum of their medical applications. The aim of our research was to synthesize and analyze the antimicrobial properties of novel 2-thiohydantoin and 2-quinolone derivatives. For this purpose, two series of hybrid compounds were synthesized. Both series consisted of 2-thiohydantoin core and 2-quinolone derivative ring, however one of them was enriched with an acetic acid group at N3 atom in 2-thiohydantoin core. Antibacterial properties of these compounds were examined against bacteria: Staphyloc

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14

Millanao, Ana R., Aracely Y. Mora, Nicolás A. Villagra, Sergio A. Bucarey, and Alejandro A. Hidalgo. "Biological Effects of Quinolones: A Family of Broad-Spectrum Antimicrobial Agents." Molecules 26, no. 23 (2021): 7153. http://dx.doi.org/10.3390/molecules26237153.

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Broad antibacterial spectrum, high oral bioavailability and excellent tissue penetration combined with safety and few, yet rare, unwanted effects, have made the quinolones class of antimicrobials one of the most used in inpatients and outpatients. Initially discovered during the search for improved chloroquine-derivative molecules with increased anti-malarial activity, today the quinolones, intended as antimicrobials, comprehend four generations that progressively have been extending antimicrobial spectrum and clinical use. The quinolone class of antimicrobials exerts its antimicrobial actions

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15

THOMAS, JULIAN M., and NEIL A. SWANSON. "Treatment of Perichondritis with a Quinolone Derivative-Norfloxacin." Journal of Dermatologic Surgery and Oncology 14, no. 4 (1988): 447–50. http://dx.doi.org/10.1111/j.1524-4725.1988.tb03381.x.

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16

Neves, Ana Rita, Fernando Durães, Joana Freitas-Silva, et al. "Derivatives of Trimethoxybenzoic Acid and Gallic Acid as Potential Efflux Pump Inhibitors: In Silico and In Vitro Studies." International Journal of Molecular Sciences 23, no. 22 (2022): 14468. http://dx.doi.org/10.3390/ijms232214468.

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The overexpression of efflux pumps is one of the strategies used by bacteria to resist antibiotics and could be targeted to circumvent the antibiotic crisis. In this work, a series of trimethoxybenzoic acid derivatives previously described as antifouling compounds was explored for potential antimicrobial activity and efflux pump (EP) inhibition. First, docking studies on the acridine resistance proteins A and B coupled to the outer membrane channel TolC (AcrAB-TolC) efflux system and a homology model of the quinolone resistance protein NorA EP were performed on 11 potential bioactive trimethox

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17

Sudhanshu Kumar Jha, Sneep Kumar Chaturvedi, Shivam Kumar Singh, et al. "Synthesis and In-silico design of a novel silver metal ciprofloxacin compound." World Journal of Advanced Research and Reviews 18, no. 1 (2023): 885–92. http://dx.doi.org/10.30574/wjarr.2023.18.1.0707.

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Ciprofloxacin is a quinolone derivative with antibacterial properties. Quinolones, which share structural similarities with nalidixic acid, function as unidentate, bidentate, and bridging ligands during chelation. A key factor in increasing quinolones' biological activity is the presence of metal ions. Many transition metals, including Ni2+, Co2+, Ca2+, Zn2+, Ag2+, Au2+, Mn2+, Mg2+, and Fe2+, are often utilised as chelating agents. The ciprofloxacin silver ions was developed in the current study and then compared with two standard medications (ciprofloxacin and norfloxacin) and evaluated for i

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18

Kwon, Chul-Wook, Young-Suck Ro, Jae-Hong Kim, So-Yun Cho, Hyung-Chul Kang, and Jeong-Hee Hahm. "Clinical Study on Topical Quinolone Derivative in Acne Vulgaris." Journal of Korean Society for Clinical Pharmacology and Therapeutics 2, no. 2 (1994): 160. http://dx.doi.org/10.12793/jkscpt.1994.2.2.160.

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19

Capparelli, M. V., J. E. Charris, and D. Cascio. "Crystal structure of a quinolone derivative with antimalarial activity." Acta Crystallographica Section A Foundations of Crystallography 49, s1 (1993): c131. http://dx.doi.org/10.1107/s0108767378096221.

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20

Kataria, Meenal, Manoj Kumar, and Vandana Bhalla. "Supramolecular Ensemble of Tetraphenylcyclopentadienone Derivative and HgO nanoparticles: A One-Pot Approach for the Synthesis of Quinoline and Quinolone Derivatives." ChemistrySelect 2, no. 10 (2017): 3018–27. http://dx.doi.org/10.1002/slct.201602069.

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21

Jantová, Soňa, Dominika Topoľská, Michaela Janošková, Miroslav Pánik, and Viktor Milata. "Original Article. Study of the cytotoxic/toxic potential of the novel anticancer selenodiazoloquinolone on fibroblast cells and 3D skin model." Interdisciplinary Toxicology 9, no. 3-4 (2016): 106–12. http://dx.doi.org/10.1515/intox-2016-0014.

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Abstract The new synthetically prepared quinolone derivative 7-ethyl 9-ethyl-6-oxo-6,9-dihydro[1,2,5]selenadiazolo [3,4-h]quinoline-7-carboxylate (E2h) showed in our previous study cytotoxic effects towards tumor cells and immunomodulatory activities on RAW 264.7 cell line murine macrophages. E2h may have a potential use as a novel chemotherapeutic agent with immunomodulatory properties and the ability to induce apoptotic death of cancer cells. The aim of the present study was to examine the antiproliferative/cytotoxic activities of E2h on human non-cancer fibroblast BHNF-1 cells and reconstru

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22

Firdaus, Irvan Maulana, Mutista Hafshah, Ahmad Faqih Amin, and Daffa Faiq Aji Satriya. "Modelling of QSAR Equations for Styryl Quinolone Compound Derivatives as HIV-1 Inhibitors." Walisongo Journal of Chemistry 7, no. 1 (2024): 107–25. https://doi.org/10.21580/wjc.v7i1.22315.

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HIV-1 (Human Immunodeficiency Virus) inhibitor compounds have been designed using a QSAR analysis approach for 33 styryl quinolone derivative compounds, with descriptors calculated using semi-empirical methods. This research aims to determine the best semi-empirical method and to obtain the best QSAR equation by comparing the Principal Component Regression method with Multiple Linear Regression, as well as modifying the structure of new styryl quinolone derivative compounds to achieve higher predicted theoretical HIV-1 integrase protein inhibitor activity. The analysis results showed that the

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23

Aldred, Katie J., Tim R. Blower, Robert J. Kerns, James M. Berger, and Neil Osheroff. "Fluoroquinolone interactions withMycobacterium tuberculosisgyrase: Enhancing drug activity against wild-type and resistant gyrase." Proceedings of the National Academy of Sciences 113, no. 7 (2016): E839—E846. http://dx.doi.org/10.1073/pnas.1525055113.

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Mycobacterium tuberculosisis a significant source of global morbidity and mortality. Moxifloxacin and other fluoroquinolones are important therapeutic agents for the treatment of tuberculosis, particularly multidrug-resistant infections. To guide the development of new quinolone-based agents, it is critical to understand the basis of drug action againstM. tuberculosisgyrase and how mutations in the enzyme cause resistance. Therefore, we characterized interactions of fluoroquinolones and related drugs with WT gyrase and enzymes carrying mutations at GyrAA90and GyrAD94.M. tuberculosisgyrase lack

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24

Sudhanshu, Kumar Jha, Kumar Chaturvedi Sneep, Kumar Singh Shivam, et al. "Synthesis and In-silico design of a novel silver metal ciprofloxacin compound." World Journal of Advanced Research and Reviews 18, no. 1 (2023): 885–92. https://doi.org/10.5281/zenodo.8176633.

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Ciprofloxacin is a quinolone derivative with antibacterial properties. Quinolones, which share structural similarities with nalidixic acid, function as unidentate, bidentate, and bridging ligands during chelation. A key factor in increasing quinolones' biological activity is the presence of metal ions. Many transition metals, including Ni<sup>2+</sup>, Co<sup>2+</sup>, Ca<sup>2+</sup>, Zn<sup>2+</sup>, Ag<sup>2+</sup>, Au<sup>2+</sup>, Mn<sup>2+</sup>, Mg<sup>2+</sup>, and Fe<sup>2+</sup>, are often utilised as chelating agents. The ciprofloxacin silver ions was developed in the current st

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25

Kimber, Marc C., Jason P. Geue, Stephen F. Lincoln, A. David Ward, and Edward R. T. Tiekink. "A Preparative and Preliminary Spectroscopic Study of Analogues of a Zinquin-Related Fluorophore." Australian Journal of Chemistry 56, no. 1 (2003): 39. http://dx.doi.org/10.1071/ch01071.

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The syntheses of the 4- and 5-methoxy isomers of 4-N-(6-methoxy-2-methyl-8-quinolyl)-4-methylbenzenesulfon-amide and of N-(2-methoxy-8-quinolyl)-4-methylbenzenesulfonamide are described. The 6-methoxy compound is a precursor of Zinquin ester, a specific fluorophore for Zn(II). The 2-methoxy analogue was synthesized by nitration of 2-chloroquinoline and subsequent functional group manipulation. The 4-methoxy isomer was synthesized from a 4-quinolone derivative, and the 5-methoxy isomer was synthesized by a standard Skraup quinoline synthesis. The structures of the 4- and 5-methoxy isomers were

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26

Gras, Jordi, Ignasi Cardelûs, Jorge Beleta, Robert Gristwood, José Maria Palacios, and Jesús Llenas. "Pharmacological Profile of LAS 31180, a New Inotropic/Vasodilator Quinolone Derivative." Arzneimittelforschung 50, no. 11 (2011): 980–86. http://dx.doi.org/10.1055/s-0031-1300321.

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27

Finch, R., J. Martin, and R. Pilkington. "In-vitro assessment of lomefloxacin (SC-47111)—a new quinolone derivative." Journal of Antimicrobial Chemotherapy 22, no. 6 (1988): 881–84. http://dx.doi.org/10.1093/jac/22.6.881.

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28

Ince, Dilek, and David C. Hooper. "Mechanisms and Frequency of Resistance to Gatifloxacin in Comparison to AM-1121 and Ciprofloxacin inStaphylococcus aureus." Antimicrobial Agents and Chemotherapy 45, no. 10 (2001): 2755–64. http://dx.doi.org/10.1128/aac.45.10.2755-2764.2001.

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ABSTRACT Gatifloxacin, an 8-methoxyfluoroquinolone, was found to be two- to fourfold more active against wild-typeStaphylococcus aureus ISP794 than its desmethoxy derivative, AM-1121, and ciprofloxacin, another desmethoxy fluoroquinolone. Single grlBA mutations caused two- to fourfold increases in the MIC of gatifloxacin, and a single gyrase mutation was silent. Double mutations in gyrA andgrlA or grlB caused a 32-fold increase in the MIC of gatifloxacin, in contrast to a 128-fold increase for ciprofloxacin and AM-1121. Overexpression of the NorA efflux pump had minimal effect on the MIC of ga

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29

Engler, Michael, Guido Rüsing, Fritz Sörgel, and Ulrike Holzgrabe. "Defluorinated Sparfloxacin as a New Photoproduct Identified by Liquid Chromatography Coupled with UV Detection and Tandem Mass Spectrometry." Antimicrobial Agents and Chemotherapy 42, no. 5 (1998): 1151–59. http://dx.doi.org/10.1128/aac.42.5.1151.

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ABSTRACT Photodegradation of sparfloxacin was observed by means of high-pressure liquid chromatography with UV detection and liquid chromatography coupled with UV detection and tandem mass spectrometry (LC-MS/MS). Three products were detected. Comparison with an independently synthesized derivative of sparfloxacin revealed the structure of one product which is believed to be 8-desfluorosparfloxacin. The second product is likely to be formed by the splitting off of a fluorine and a cyclopropyl ring. Thus, photodefluorination of quinolone antibacterial agents is found and proved for the first ti

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30

B. Bakare, S. "Synthesis and biological evaluation of some hybrid 2-quinolinone derivatives containing cinnamic acid as anti-breast cancer drugs." Bulletin of the Chemical Society of Ethiopia 35, no. 3 (2022): 551–64. http://dx.doi.org/10.4314/bcse.v35i3.7.

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ABSTRACT. A new series of hybrid 2-quinolinone derivatives were synthesized by using 7-hydroxy-4-methyl-1-amino-quinolin-2-one (2) and cinnamic acid. Hybrid halogenated 2-quinolinone derivatives (3-(7-hydroxy-4-methyl-3,6,8-tribromo-2-oxo-2H-quinolin-1-ylamino)-3-phenyl acrylic acid (4) and 3-(7-acetoxy-4-methyl-3,6,8-tribromo-2-oxo-1H-quinolin-1-ylamino)-3-phenyl acrylic acid (7)) were prepared via the halogenation of 3-(7-hydroxy-4-methyl-2-oxo-2H-quinolin-1-ylamino)-3-phenyl acrylic acid (3) with bromine to give compound 4 with acetic anhydride led to the formation of hydride halogenated 2-

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31

Wada, K., A. R. Saniahadi, K. Umemura, Y. Takiguchi, and M. Nakashima. "UV-Dependent Quinolone-Induced Human Erythrocyte Membrane Lipid Peroxidation: Studies on the Phototoxicity of Y-26611, a New Quinolone Derivative." Pharmacology & Toxicology 74, no. 6 (1994): 240–43. http://dx.doi.org/10.1111/j.1600-0773.1994.tb01105.x.

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32

Molnár, Kinga, Bálint Lőrinczi, Csilla Fazakas, et al. "SZR-104, a Novel Kynurenic Acid Analogue with High Permeability through the Blood–Brain Barrier." Pharmaceutics 13, no. 1 (2021): 61. http://dx.doi.org/10.3390/pharmaceutics13010061.

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By being an antagonist of glutamate and other receptors, kynurenic acid serves as an endogenous neuroprotectant in several pathologies of the brain. Unfortunately, systemic administration of kynurenic acid is hindered by its low permeability through the blood–brain barrier. One possibility to overcome this problem is to use analogues with similar biological activity as kynurenic acid, but with an increased permeability through the blood–brain barrier. We synthesized six novel aminoalkylated amide derivatives of kynurenic acid, among which SZR-104 (N-(2-(dimethylamino)ethyl)-3-(morpholinomethyl

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33

Alini, S., A. Citterio, A. Farina, M. C. Fochi, and L. Malpezzi. "3,4,4a,5,6,7,8,8a-Octahydro-8a-hydroxy-2-quinolone and its 8a-Hydroperoxy Derivative." Acta Crystallographica Section C Crystal Structure Communications 54, no. 7 (1998): 1000–1003. http://dx.doi.org/10.1107/s0108270198001565.

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34

Ikeda, Satoru, Masashi Yazawa, and Chiaki Nishimura. "Antiviral activity and inhibition of topoisomerase by ofloxacin, a new quinolone derivative." Antiviral Research 8, no. 3 (1987): 103–13. http://dx.doi.org/10.1016/0166-3542(87)90064-7.

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35

Saleh, Ahmad, Johannes Friesen, Stefan Baumeister, Uwe Gross, and Wolfgang Bohne. "Growth Inhibition of Toxoplasma gondii and Plasmodium falciparum by Nanomolar Concentrations of 1-Hydroxy-2-Dodecyl-4(1H)Quinolone, a High-Affinity Inhibitor of Alternative (Type II) NADH Dehydrogenases." Antimicrobial Agents and Chemotherapy 51, no. 4 (2007): 1217–22. http://dx.doi.org/10.1128/aac.00895-06.

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ABSTRACT Both apicomplexan parasites Toxoplasma gondii and Plasmodium falciparum lack type I NADH dehydrogenases (complex I) but instead carry alternative (type II) NADH dehydrogenases, which are absent in mammalian cells and are thus considered promising antimicrobial drug targets. The quinolone-like compound 1-hydroxy-2-dodecyl-4(1H)quinolone (HDQ) was recently described as a high-affinity inhibitor of fungal alternative NADH dehydrogenases in enzymatic assays, probably by interfering with the ubiquinol binding site of the enzyme. We describe here that HDQ effectively inhibits the replicatio

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Xie, Jian-Wu, Jia-Wen Zhang, Li-Si-Han Yu, Jian-Lian Dong, and Qi-Chao Sun. "Enantioselective Construction and Transformations of Polyfunctionalized 3,4-Dihydro-2H-thiopyrano[2,3-b]quinolines." Synlett 29, no. 05 (2017): 603–8. http://dx.doi.org/10.1055/s-0036-1591838.

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We developed an enantioselective organocascade Michael/Henry reaction in the presence of a bifunctional organocatalyst to construct chiral polyfunctionalized 3,4-dihydro-2H-thiopyrano[2,3-b]quinolines. The resulting optically active products with three contiguous stereocenters, one quaternary and two tertiary, were obtained in moderate to good yields and with good to excellent enantioselectivities. Remarkably, the resulting products were readily converted into polyfunctionalized optically active furo[2′,3′:4,5]thiopyrano[2,3-b]quinoline, 3,4-dihydro-2H-thiopyrano[2,3-b]quinoline 1-oxide and 2,

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Peng, Lizeng, Tao Zhang, Ying Li, and Yulin Li. "SYNTHESIS OF PYRAZOLE DERIVATIVES 4(1H)-QUINOLONE AND 4-CHLOROQUINOLINE BY THERMOLYSIS OF ARYLAMINOMETHYLENE MELDRUM's ACID DERIVATIVE." Synthetic Communications 32, no. 5 (2002): 785–91. http://dx.doi.org/10.1081/scc-120002520.

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Himbert, Gerhard, and Oliver Gerulat. "Einige Umsetzungen von Inhydrazinen mit Isocyanaten: [2+2]- und [4+2]Cycloadditionen, (Hydrazinoethinyl)metallierung / Some Reactions of Ynehydrazines with Isocyanates: [2+2]- and [4+2]Cycloadditions, (Hydrazinoethynyl)metallation." Zeitschrift für Naturforschung B 56, no. 11 (2001): 1196–204. http://dx.doi.org/10.1515/znb-2001-1115.

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The (silylethynyl)- and the (tolylethinyl)-hydrazines 1a and 1b react with aryl isocyanates 2a-e and arylsulfonyl isocyanates 2f,g to form the corresponding substituted 3-arylimino-(or arylsulfonylimino-) 1,1,2-trimethyl-5-oxopyrazolidinium-4-ides 3a-h. The silyl group in the 4-position can be replaced by a hydrogen atom (formation of 6a-e). Heating of 6d in toluene induced the unequivocal transformation of the betaine to an isomer, the spectrocopic data of which are in concordance with those of the 4-quinolone derivative 7. Aroyl isocyanates 8 react in a [4+2]cycloaddition with la to furnish

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Kumar, Anil, Nishtha Saxena, Arti Mehrotra, and Nivedita Srivastava. "Review: Studies on the Synthesis of Quinolone Derivatives with Their Antibacterial Activity (Part 1)." Current Organic Chemistry 24, no. 8 (2020): 817–54. http://dx.doi.org/10.2174/1385272824999200427082108.

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Quinolone derivatives have attracted considerable attention due to their medicinal properties. This review covers many synthetic routes of quinolones preparation with their antibacterial properties. Detailed study with structure-activity relationship among quinolone derivatives will be helpful in designing new drugs in this field.

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Balaji, Swapnaa, Rabin Neupane, Chandrabose Karthikeyan, Jayachandra Babu Ramapuram, and Amit K. Tiwari. "Abstract 4974: Development of novel pyrimido-pyrazolo-quinolone derivative, IND-2 as multi-targeted inhibitor for the treatment of prostate cancer." Cancer Research 83, no. 7_Supplement (2023): 4974. http://dx.doi.org/10.1158/1538-7445.am2023-4974.

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Abstract Prostate cancer (PC) is the most commonly diagnosed cancer in men. In PC, multiple molecular signaling networks are perturbed, so monotherapies are less effective, creating an urgent need to discover chemotherapeutic agents that target multiple tumor-promoting proteins simultaneously. Drug discovery research is increasingly embracing poly-pharmacology, in which one drug targets multiple oncogenic targets concurrently. We have identified a novel quinoline derivative, IND-2 (4-chloro-2-methylpyrimido[1″,2″:1,5]pyrazolo[3,4-b]quinolone), that has been shown to significantly inhibit the e

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Hawtin, Rachael E., David E. Stockett, Jo Ann W. Byl, et al. "Voreloxin Is an Anticancer Quinolone Derivative that Intercalates DNA and Poisons Topoisomerase II." PLoS ONE 5, no. 4 (2010): e10186. http://dx.doi.org/10.1371/journal.pone.0010186.

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Norrby, S. R., and M. Jonsson. "Comparative in vitro activity of PD 127,391, a new fluorinated 4-quinolone derivative." Antimicrobial Agents and Chemotherapy 32, no. 8 (1988): 1278–81. http://dx.doi.org/10.1128/aac.32.8.1278.

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Digranes, Asbjørn, Eva Benonisen, Aud Salveson, and Friederike Zahm. "In vitro Studies of Fleroxacin (Ro 23-6240), a New Trifluorinated Quinolone Derivative." Chemotherapy 34, no. 5 (1988): 401–10. http://dx.doi.org/10.1159/000238599.

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Ranjith, P. K., Y. Sheena Mary, C. Yohannan Panicker, et al. "New quinolone derivative: Spectroscopic characterization and reactivity study by DFT and MD approaches." Journal of Molecular Structure 1135 (May 2017): 1–14. http://dx.doi.org/10.1016/j.molstruc.2017.01.045.

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Sofuni, T., M. Kawase, H. Mizusawa, et al. "Induction of chromosome-type aberrations by a quinolone derivative in cultured mammalian cells." Mutation Research/Environmental Mutagenesis and Related Subjects 252, no. 1 (1991): 108. http://dx.doi.org/10.1016/0165-1161(91)90316-z.

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Sonawane, Amol D., Dinesh R. Garud, Taro Udagawa, and Mamoru Koketsu. "Synthesis of thieno[2,3-b]quinoline and selenopheno[2,3-b]quinoline derivativesviaiodocyclization reaction and a DFT mechanistic study." Organic & Biomolecular Chemistry 16, no. 2 (2018): 245–55. http://dx.doi.org/10.1039/c7ob02523h.

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Thieno[2,3-b]quinoline and selenopheno[2,3-b]quinoline derivatives were synthesized by the regioselective iodocyclization reaction of 3-alkynyl-2-(methylthio)quinolines and 3-alkynyl-2-(methylseleno)quinolines.

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Tian, Juan Juan, Xin Zhou, Hui Juan Hao, and Xue Wu. "A Highly Selective and Sensitive Fluorescent Probe Based on Quinolone Derivative for Hg²⁺ in Aqueous Solution." Advanced Materials Research 549 (July 2012): 229–33. http://dx.doi.org/10.4028/www.scientific.net/amr.549.229.

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A new fluorescent probe, quinoline derivative DPQ bearing a methyl pyrrolidine-1-carbodithioate group, was synthesized and characterized by IR, Tof-MS and NMR. Its fluorescent behaviors toward transition metal ions were investigated. The results indicate that DPQ shows unique selective and high sensitive for Hg2+ in aqueous solution with a broad pH range 4-10. DPQ forms a 1:2 metal-ligand complex with Hg2+ ions with a limit of detection as low as 1.7×10-6 mol/L.

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Mollova-Sapundzhieva, Yordanka, Plamen Angelov, Danail Georgiev та Pavel Yanev. "Synthetic approach to 2-alkyl-4-quinolones and 2-alkyl-4-quinolone-3-carboxamides based on common β-keto amide precursors". Beilstein Journal of Organic Chemistry 19 (23 листопада 2023): 1804–10. http://dx.doi.org/10.3762/bjoc.19.132.

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β-Keto amides were used as convenient precursors to both 2-alkyl-4-quinolones and 2-alkyl-4-quinolone-3-carboxamides. The utility of this approach is demonstrated with the synthesis of fourteen novel and four known quinolone derivatives, including natural products of microbial origin such as HHQ and its C5-congener. Two compounds with high activity against S. aureus have been identified among the newly obtained quinolones, with MICs ≤ 3.12 and ≤ 6.25 µg/mL, respectively.

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Bergamini, F. R. G., M. A. Ribeiro, P. C. M. L. Miranda, A. L. B. Formiga, and P. P. Corbi. "A novel binuclear copper complex incorporating a nalidixic acid derivative displaying a one-dimensional coordination polymeric structure." Acta Crystallographica Section C Structural Chemistry 72, no. 7 (2016): 544–48. http://dx.doi.org/10.1107/s2053229616008913.

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The identification of the antibacterial action of nalidixic acid (nx) was central to the development of the quinolone antibacterial compounds. The ability of the nx naphthyridyl ring to interact with and inhibit some proteins has encouraged the investigation of similar structures in the search for more active compounds with less adverse effects. The possibility of structural modification by attachment of other biologically active moieties to the naphthyridyl ring of nx allowed the development of new active antimicrobial molecules. Hydrazone derivatives of nx can be synthesized easily based on

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Gravina, Giovanni Luca, Andrea Mancini, Claudia Mattei, et al. "Enhancement of radiosensitivity by the novel anticancer quinolone derivative vosaroxin in preclinical glioblastoma models." Oncotarget 8, no. 18 (2017): 29865–86. http://dx.doi.org/10.18632/oncotarget.16168.

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