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1

Nqoro, Xhamla, and Blessing A. Aderibigbe. "4-Aminoquinoline-ferrocene Hybrids as Potential Antimalarials." Recent Patents on Anti-Infective Drug Discovery 15, no. 2 (2020): 157–72. http://dx.doi.org/10.2174/1574891x15666200804160322.

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Background: Malaria is a deadly disease. It is mostly treated using 4- aminoquinoline derivatives such as chloroquine etc. because it is well-tolerated, displays low toxicity, and after administration, it is rapidly absorbed. The combination of 4-aminoquinoline with other classes of antimalarial drugs has been reported to be an effective approach for the treatment of malaria. Furthermore, some patents reported hybrids 4-aminoquinolines containing ferrocene moiety with potent antimalarial activity. Objective: The objective of the current study is to prepare 4-aminoquinoline-ferrocene hybrids vi
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2

Lokaj, Jan, Viktor Kettmann, Petra Černuchová, Viktor Milata, and Marek Fronc. "3-Acetyl-4-aminoquinoline." Acta Crystallographica Section E Structure Reports Online 63, no. 3 (2007): o1164—o1166. http://dx.doi.org/10.1107/s1600536807004746.

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The title compound, C11H10N2O, a potential antitumour drug, crystallizes with two molecules in the asymmetric unit. The 4-amino N atom is strongly conjugated with the quinoline ring involving the 3-carbonyl group. As a result, the molecule is almost planar. The amino group is involved in both intramolecular N—H...O and intermolecular N—H...N hydrogen bonds.
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3

Sáenz, Fabián E., Tina Mutka, Kenneth Udenze, Ayoade M. J. Oduola, and Dennis E. Kyle. "Novel 4-Aminoquinoline Analogs Highly Active against the Blood and Sexual Stages of PlasmodiumIn VivoandIn Vitro." Antimicrobial Agents and Chemotherapy 56, no. 9 (2012): 4685–92. http://dx.doi.org/10.1128/aac.01061-12.

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ABSTRACTNew drugs to treat malaria must act rapidly and be highly potent against asexual blood stages, well tolerated, and affordable to residents of regions of endemicity. This was the case with chloroquine (CQ), a 4-aminoquinoline drug used for the prevention and treatment of malaria. However, since the 1960s,Plasmodium falciparumresistance to this drug has spread globally, and more recently, emerging resistance to CQ byPlasmodium vivaxthreatens the health of 70 to 320 million people annually. Despite the emergence of CQ resistance, synthetic quinoline derivatives remain validated leads for
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4

Dolengovski, Egor L., Tatyana V. Gryaznova, Oleg G. Sinyashin, Elena L. Gavrilova, Kirill V. Kholin, and Yulia H. Budnikova. "Morpholine Radical in the Electrochemical Reaction with Quinoline N-Oxide." Catalysts 13, no. 9 (2023): 1279. http://dx.doi.org/10.3390/catal13091279.

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An electrochemical reaction between quinoline N-oxides and morpholine was developed by using Cu(OAc)2 as a catalyst, generating products of 4-aminoquinoline N-oxides in CH2Cl2 or 2-aminoquinoline N-oxides in CH3CN in good yields. With an increase in the amount of electricity passed, the product deoxygenates with the formation of aminoquinolines. The advantages of the reaction are mild conditions, room temperature, the use of morpholine rather than its derivatives, and the ability to control the process when the electrolysis conditions change. Bisubstituted quinoline has also been obtained. The
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5

Opsenica, Igor, Kirsten Smith, Lucia Gerena, Sandra Gaica, and Bogdan Solaja. "Ribofuranose as a carrier of tetraoxane and 4-aminoquinoline antimalarial pharmacophores." Journal of the Serbian Chemical Society 73, no. 11 (2008): 1021–25. http://dx.doi.org/10.2298/jsc0811021o.

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Several tetraoxane and 4-aminoquinoline molecules were prepared in order to examine the influence of ribofuranose as a carrier molecule on the antimalarial activity of test compounds. The synthesized compounds showed pronounced antimalarial activity against Plasmodium falciparum chloroquine susceptible D6, chloroquine resistant W2 and multidrug-resistant TM91C235 (Thailand) strains. The aminoquinoline derivative 4 was more active against W2 and TM91C235 strains than the control compounds (CQ and MFQ).
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6

Hadanu, Ruslin, Chairil Anwar, Jumina Jumina, Iqmal Tahir, and Mustofa Mustofa. "SYNTHESIS OF ANTIMALARIAL 3-(2-HYDROXYETHYL)-2-METHYL-1,10-PHENANTHROLINE-4-OL FROM 8-AMINOQUINOLINE." Indonesian Journal of Chemistry 4, no. 2 (2010): 82–87. http://dx.doi.org/10.22146/ijc.21858.

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It has been conducted the synthesis of 3-(2-hydroxyethyl)-2-methyl-1,10-phenanthroline-4-ol was carried out from 8-aminoquinoline which are expected to posses antimalarial activity. The experiment perfomed consisted of two steps i.e (1) reaction of 8-aminoquinoline with 2-acetyl-butyrolactone and (2) cyclization of the resulted 3-[1-(quinolin-8-ylamino)-ethylidene]-4,5-dihydro-furan-2-one. The reaction of 8-aminoquinoline with 2-acetyl-butyrolactone was performed in toluene at reflux for 6 hours in the presence of p-toluensulfonic acid as catalyst. This reaction gave 3-[1-(quinolin-8-ilamino)-
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7

Médebielle, Maurice, Stéphane Hohn, Etsuji Okada, Hidehiko Myoken, and Dai Shibata. "Synthesis of novel fluorinated 4-aminoquinoline derivatives." Tetrahedron Letters 46, no. 45 (2005): 7817–21. http://dx.doi.org/10.1016/j.tetlet.2005.09.018.

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8

Vaiana, Nadia, Melissa Marzahn, Silvia Parapini, et al. "Antiplasmodial activities of 4-aminoquinoline–statine compounds." Bioorganic & Medicinal Chemistry Letters 22, no. 18 (2012): 5915–18. http://dx.doi.org/10.1016/j.bmcl.2012.07.069.

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9

Antinarelli, Luciana M. R., Rafael M. P. Dias, Isabela O. Souza, et al. "4-Aminoquinoline Derivatives as Potential Antileishmanial Agents." Chemical Biology & Drug Design 86, no. 4 (2015): 704–14. http://dx.doi.org/10.1111/cbdd.12540.

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10

Yunnikova, L. P., Yu E. Likhareva, and V. V. Esenbaeva. "Electrophilic Tropylation of Aminopyridines and 4-Aminoquinoline." Russian Journal of General Chemistry 89, no. 9 (2019): 1927–30. http://dx.doi.org/10.1134/s1070363219090305.

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11

Manohar, Sunny, Shabana I. Khan, and Diwan S. Rawat. "Synthesis of 4-aminoquinoline-1,2,3-triazole and 4-aminoquinoline-1,2,3-triazole-1,3,5-triazine Hybrids as Potential Antimalarial Agents." Chemical Biology & Drug Design 78, no. 1 (2011): 124–36. http://dx.doi.org/10.1111/j.1747-0285.2011.01115.x.

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12

Živanović, Marija, Milica Selaković, Aleksandar Pavić, et al. "Unveiling the 4-aminoquinoline derivatives as potent agents against pancreatic ductal adenocarcinoma (PDAC) cell lines." Chemico-Biological Interactions 404 (December 7, 2024): 111281. https://doi.org/10.1016/j.cbi.2024.111281.

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Abstract Common antimalarials such as artemisinins, chloroquine and their derivatives also possess potent anti-inflamantory, antiviral and anticancer properties. In the search for new therapeutics to combat difficult-to-treat pancreatic carcinomas, we unveiled that 4-aminoquinoline derivatives, with significant antiplasmodial properties and a great safety profile&nbsp;<em>in vivo</em>, have remarkable anticancer activity against pancreatic ductal adenocarcinoma (PDAC) and considerable efficacy in the xenograft model&nbsp;<em>in vivo</em>. The aim of the present study was to further investigate
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13

Sanap, Anita Kailas, and Ganapati Subray Shankarling. "Environmentally benign synthesis of 4-aminoquinoline-2-ones using recyclable choline hydroxide." New Journal of Chemistry 39, no. 1 (2015): 206–12. http://dx.doi.org/10.1039/c4nj01281j.

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14

Singh, Priyanka, and Tamanna Narsinghani. "Comprehensive review on hybridization approach in anti-malarial research." INDIAN JOURNAL OF HETEROCYCLIC CHEMISTRY 34, no. 03 (2024): 407. http://dx.doi.org/10.59467/ijhc.2024.34.407.

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Malaria endures a major health problem worldwide. Over the past few decades, the issue posed by multidrug resistance has reached an alarming level in many countries. The use of most anti-malarial agents is limited not only by the rapid development of drug resistance but also by the measured pipeline of effective pharmaceuticals available against resistant strains. Hybrid molecules, which contain multiple pharmacophoric units covalently linked together through metabolically stable linkage (conjugate), fusion, and merging of two functionalities into single molecule have the prospects to conquer
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15

Kathiravan, Muthu Kumaradoss. "Molecular modelling investigation on 4-aminoquinoline derivatives as potent anti-tubercular agents." Journal of medical pharmaceutical and allied sciences 11, no. 5 (2022): 5304–11. http://dx.doi.org/10.55522/jmpas.v11i5.4167.

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The emergency of new Mycobacterium tuberculosis strains leads to multi-drug resistant tuberculosis (MDR) and total drug resistant tuberculosis (TDR) indicating the urgency in the development of newer anti-tubercular agents to be effective against the resistance strains. In the present study pharmacophore modelling and atom-based 3D-QSAR of 4-Aminoquinoline derivatives was carried out to understand the key structural features responsible for anti-tb activity. Phase module of Schrödinger was used to generate a five-point Pharmacophore for 46 molecules belonging to 4-Aminoquinolines. The best sco
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16

Glanzmann, Nicolas, Thamara Kelcya F. Oliveira, Vinicius Carius de Souza, et al. "Potent and selective inhibitory effect of 4-aminoquinoline derivatives on SARS-CoV-2 replication." Innovative Medicines & Omics 1, no. 1 (2024): 3442. http://dx.doi.org/10.36922/imo.3442.

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The global coronavirus disease 2019 (COVID-19) pandemic, caused by the highly infectious severe acute respiratory syndrome coronavirus 2 (SARS-CoV-2), had resulted in significant mortality worldwide. In 2020, the World Health Organization started the solidarity clinical trial to assess the efficacy of four proposed therapeutic strategies, including chloroquine (CQ), a 4-aminoquinoline molecule. However, CQ lacks clinical benefit and, therefore, failed to show in vitro anti-SARS-CoV-2 activity in TMPRSS2-expressing cells, such as Calu-3 cell line, which recapitulate human type II pneumocytes. N
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17

Kumar, Deepak, Shabana I. Khan, Babu L. Tekwani, Prija Ponnan, and Diwan S. Rawat. "Synthesis, antimalarial activity, heme binding and docking studies of 4-aminoquinoline–pyrimidine based molecular hybrids." RSC Adv. 4, no. 109 (2014): 63655–69. http://dx.doi.org/10.1039/c4ra09768h.

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18

Aderibigbe, B. A., and E. W. Neuse. "Macromolecular Conjugates of 4- and 8-Aminoquinoline Compounds." Journal of Inorganic and Organometallic Polymers and Materials 22, no. 2 (2011): 429–38. http://dx.doi.org/10.1007/s10904-011-9616-1.

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19

McCall, John M., R. E. TenBrink, Bharat V. Kamdar, et al. "7-(Trifluoromethyl)-4-aminoquinoline hypotensives: novel peripheral sympatholytics." Journal of Medicinal Chemistry 29, no. 1 (1986): 133–37. http://dx.doi.org/10.1021/jm00151a021.

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20

Komatović, Katarina, Ana Matošević, Nataša Terzić-Jovanović, et al. "4-Aminoquinoline-Based Adamantanes as Potential Anticholinesterase Agents in Symptomatic Treatment of Alzheimer’s Disease." Pharmaceutics 14, no. 6 (2022): 1305. http://dx.doi.org/10.3390/pharmaceutics14061305.

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Considering that acetylcholinesterase (AChE) inhibition is the most important mode of action expected of a potential drug used for the treatment of symptoms of Alzheimer’s disease (AD), our previous pilot study of 4-aminoquinolines as potential human cholinesterase inhibitors was extended to twenty-two new structurally distinct 4-aminoquinolines bearing an adamantane moiety. Inhibition studies revealed that all of the compounds were very potent inhibitors of AChE and butyrylcholinesterase (BChE), with inhibition constants (Ki) ranging between 0.075 and 25 µM. The tested compounds exhibited a m
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21

Thakur, Anuj, Shabana I. Khan, and Diwan S. Rawat. "Synthesis of piperazine tethered 4-aminoquinoline-pyrimidine hybrids as potent antimalarial agents." RSC Adv. 4, no. 40 (2014): 20729–36. http://dx.doi.org/10.1039/c4ra02276a.

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22

Manohar, Sunny, V. Satya Pavan, Dale Taylor, et al. "Highly active 4-aminoquinoline–pyrimidine based molecular hybrids as potential next generation antimalarial agents." RSC Advances 5, no. 36 (2015): 28171–86. http://dx.doi.org/10.1039/c4ra16032k.

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23

Yuan, Jing-Mei, Nan-Ying Chen, Hao-Ran Liao, et al. "3-(Benzo[d]thiazol-2-yl)-4-aminoquinoline derivatives as novel scaffold topoisomerase I inhibitor via DNA intercalation: design, synthesis, and antitumor activities." New Journal of Chemistry 44, no. 26 (2020): 11203–14. http://dx.doi.org/10.1039/c9nj05846j.

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24

Ruiz, Jérémy, Sonia Mallet-Ladeira, Marjorie Maynadier, Henri Vial, and Christiane André-Barrès. "Design, synthesis and evaluation of new tricyclic endoperoxides as potential antiplasmodial agents." Org. Biomol. Chem. 12, no. 28 (2014): 5212–21. http://dx.doi.org/10.1039/c4ob00787e.

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25

Chen, Yao, Yaoyao Bian, Yuan Sun, et al. "Identification of 4-aminoquinoline core for the design of new cholinesterase inhibitors." PeerJ 4 (July 7, 2016): e2140. http://dx.doi.org/10.7717/peerj.2140.

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Inhibition of acetylcholinesterase (AChE) using small molecules is still one of the most successful therapeutic strategies in the treatment of Alzheimer’s disease (AD). Previously we reported compound T5369186 with a core of quinolone as a new cholinesterase inhibitor. In the present study, in order to identify new cores for the designing of AChE inhibitors, we screened different derivatives of this core with the aim to identify the best core as the starting point for further optimization. Based on the results, we confirmed that only 4-aminoquinoline (compound 04 and 07) had cholinesterase inh
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26

Raj, Raghu, Kirkwood M. Land, and Vipan Kumar. "4-Aminoquinoline-hybridization en route towards the development of rationally designed antimalarial agents." RSC Advances 5, no. 101 (2015): 82676–98. http://dx.doi.org/10.1039/c5ra16361g.

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27

Gan, Zixu, Ke Zhang, Peng Shi, Yingsheng Zhao та Runsheng Zeng. "Copper(i)-catalyzed radical carboamination reaction of 8-aminoquinoline-oriented buteneamides with chloroform: synthesis of-β-lactams". RSC Advances 11, № 45 (2021): 28081–84. http://dx.doi.org/10.1039/d1ra05233k.

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28

Hisamatsu, Yosuke, Naoki Umezawa, Hirokazu Yagi, Koichi Kato, and Tsunehiko Higuchi. "Design and synthesis of a 4-aminoquinoline-based molecular tweezer that recognizes protoporphyrin IX and iron(iii) protoporphyrin IX and its application as a supramolecular photosensitizer." Chemical Science 9, no. 38 (2018): 7455–67. http://dx.doi.org/10.1039/c8sc02133c.

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29

Vale, Nuno, Joana Matos, Rui Moreira, and Paula Gomes. "Electrospray Ionization Mass Spectrometry as a Valuable Tool in the Characterization of Novel Primaquine Peptidomimetic Derivatives." European Journal of Mass Spectrometry 15, no. 5 (2009): 627–40. http://dx.doi.org/10.1255/ejms.1011.

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Novel primaquine-derived antimalarials have been extensively characterized by electrospray ionization-ion trap mass spectrometry (ESI-MS). Experiments by in-source collision-induced dissociation (CID) in the nozzle–skimmer region (NSR) or by tandem mass spectrometry (MS/MS) are shown to be most valuable tools for the physico–chemical characterization of these 8-aminoquinolinic drugs that also bear the biologically relevant imidazolidin-4-one scaffold. It was possible to find parallelism between compound stability in the NSR and its reactivity towards hydrolysis at physiological pH and T. Moreo
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30

Singh, V., L. Tyagi, M. Singhal, CS Sharma, and ML Sharma. "A new generation of 7-Chloro-4-Aminoquinoline antimalarials." Systematic Reviews in Pharmacy 1, no. 2 (2010): 182. http://dx.doi.org/10.4103/0975-8453.75081.

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31

Bray, Patrick, B. Park, Egbaleh Asadollaly, et al. "A Medicinal Chemistry Perspective on 4-Aminoquinoline Antimalarial Drugs." Current Topics in Medicinal Chemistry 6, no. 5 (2006): 479–507. http://dx.doi.org/10.2174/156802606776743147.

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32

Manohar, Sunny, Mohit Tripathi, and Diwan Rawat. "4-Aminoquinoline Based Molecular Hybrids as Antimalarials: An Overview." Current Topics in Medicinal Chemistry 14, no. 14 (2014): 1706–33. http://dx.doi.org/10.2174/1568026614666140808125728.

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33

Sheng, Hui-Yang, Hui Chen, Meng Liao, et al. "Copper-catalyzed Tandem Cyclization to Access 4-Aminoquinoline Derivatives." Chemistry Letters 49, no. 5 (2020): 526–29. http://dx.doi.org/10.1246/cl.200053.

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34

Khan, M. O. Faruk, Mark S. Levi, Babu L. Tekwani, Shabana I. Khan, Eiichi Kimura, and Ronald F. Borne. "Synthesis and Antimalarial Activities of Cyclen 4-Aminoquinoline Analogs." Antimicrobial Agents and Chemotherapy 53, no. 4 (2009): 1320–24. http://dx.doi.org/10.1128/aac.01304-08.

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ABSTRACT In an attempt to augment the efficacy of 7-chloro 4-aminoquinoline analogs and also to overcome resistance to antimalarial agents, we synthesized three cyclen (1,4,7,10-tetraazacyclododecane) analogs of chloroquine [a bisquinoline derivative, 7-chloro-4-(1,4,7,10-tetraaza-cyclododec-1-yl)-quinoline HBr, and a 7-chloro-4-(1,4,7,10-tetraaza-cyclododec-1-yl)-quinoline-Zn2+ complex]. The bisquinoline displays the most potent in vitro and in vivo antimalarial activities. It displays 50% inhibitory concentrations (IC50s) of 7.5 nM against the D6 (chloroquine-sensitive) clone of Plasmodium f
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35

Sparatore, Anna, Nicoletta Basilico, Manolo Casagrande, et al. "Antimalarial activity of novel pyrrolizidinyl derivatives of 4-aminoquinoline." Bioorganic & Medicinal Chemistry Letters 18, no. 13 (2008): 3737–40. http://dx.doi.org/10.1016/j.bmcl.2008.05.042.

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36

Jiang, Jinlong, Peter Lin, Myle Hoang, et al. "4-Aminoquinoline melanin-concentrating hormone 1-receptor (MCH1R) antagonists." Bioorganic & Medicinal Chemistry Letters 16, no. 20 (2006): 5275–79. http://dx.doi.org/10.1016/j.bmcl.2006.08.008.

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37

Ren, Jie, Juan Zhao, Yong-Sheng Zhou, Xian-Hua Liu, Xin Chen, and Kun Hu. "Synthesis and antitumor activity of novel 4-aminoquinoline derivatives." Medicinal Chemistry Research 22, no. 6 (2012): 2855–61. http://dx.doi.org/10.1007/s00044-012-0283-8.

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38

Khan, B., A. D. Brandling-Bennett, W. M. Watkins, A. J. Oloo, P. Ojoo, and D. K. Koech. "Plasmodium falciparumsensitivity to erythromycin and 4-aminoquinoline combinationsin vitro." Annals of Tropical Medicine & Parasitology 85, no. 2 (1991): 215–22. http://dx.doi.org/10.1080/00034983.1991.11812548.

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39

Manohar, Sunny, Antonella Pepe, Christian E. Vélez Gerena, Beatriz Zayas, Sanjay V. Malhotra, and Diwan S. Rawat. "Anticancer activity of 4-aminoquinoline-triazine based molecular hybrids." RSC Advances 4, no. 14 (2014): 7062. http://dx.doi.org/10.1039/c3ra45333b.

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40

Sparatore, Anna, Nicoletta Basilico, Silvia Parapini, et al. "4-Aminoquinoline quinolizidinyl- and quinolizidinylalkyl-derivatives with antimalarial activity." Bioorganic & Medicinal Chemistry 13, no. 18 (2005): 5338–45. http://dx.doi.org/10.1016/j.bmc.2005.06.047.

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41

Ribeiro, Carlos J. A., S. Praveen Kumar, Jiri Gut, et al. "Squaric acid/4-aminoquinoline conjugates: Novel potent antiplasmodial agents." European Journal of Medicinal Chemistry 69 (November 2013): 365–72. http://dx.doi.org/10.1016/j.ejmech.2013.08.037.

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42

Tripathi, Mohit, Shabana I. Khan, Anuj Thakur, Prija Ponnan, and Diwan S. Rawat. "4-Aminoquinoline-pyrimidine-aminoalkanols: synthesis, in vitro antimalarial activity, docking studies and ADME predictions." New Journal of Chemistry 39, no. 5 (2015): 3474–83. http://dx.doi.org/10.1039/c5nj00094g.

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4-Aminoquinoline-pyrimidine-aminoalkanols displaying good in vitro antimalarial activities against both CQ-sensitive and -resistant strains of P. falciparum, together with favourable resistance-indices and the predicted ADME properties, are reported.
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43

Tukulula, Matshawandile, Stefan Louw, Mathew Njoroge, and Kelly Chibale. "Synthesis and In Vitro Antiprotozoan Evaluation of 4-/8-Aminoquinoline-based Lactams and Tetrazoles." Molecules 25, no. 24 (2020): 5941. http://dx.doi.org/10.3390/molecules25245941.

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A second generation of 4-aminoquinoline- and 8-aminoquinoline-based tetrazoles and lactams were synthesized via the Staudinger and Ugi multicomponent reactions. These compounds were subsequently evaluated in vitro for their potential antiplasmodium activity against a multidrug-resistant K1 strain and for their antitrypanosomal activity against a cultured T. b. rhodesiense STIB900 strain. Several of these compounds (4a–g) displayed good antiplasmodium activities (IC50 = 0.20–0.62 µM) that were comparable to the reference drugs, while their antitrypanosomal activity was moderate (&lt;20 µM). Com
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44

Yang, Feng-Lei, Xin Chen, Wen-Hao Wu, et al. "Spin switching in tris(8-aminoquinoline)iron(ii)(BPh4)2: quantitative guest-losing dependent spin crossover properties and single-crystal-to-single-crystal transformation." Dalton Transactions 48, no. 1 (2019): 231–41. http://dx.doi.org/10.1039/c8dt03584a.

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45

Vidyacharan, Shinde, A. Sagar, and Duddu S. Sharada. "A new route for the synthesis of highly substituted 4-aminoquinoline drug like molecules via aza hetero–Diels–Alder reaction." Organic & Biomolecular Chemistry 13, no. 28 (2015): 7614–18. http://dx.doi.org/10.1039/c5ob01023c.

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46

Veiga, M. I., P. E. Ferreira, M. Malmberg, et al. "pfmdr1Amplification Is Related to Increased Plasmodium falciparum In Vitro Sensitivity to the Bisquinoline Piperaquine." Antimicrobial Agents and Chemotherapy 56, no. 7 (2012): 3615–19. http://dx.doi.org/10.1128/aac.06350-11.

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ABSTRACTThe 4-aminoquinoline bisquinoline piperaquine is an important partner drug in one of the presently recommended artemisinin combination therapies. Recent clinical trials have confirmed its high efficacy in combination with dihydroartemisinin. Resistance to piperaquine alone has, however, been documented. Amplification in copy number of thePlasmodium falciparummultidrug resistance locus on chromosome 5, containing thepfmdr1gene, has been shown to confer resistance to structurally unrelated antimalarials. Through the determination of the 50% inhibitory concentrations (IC50s) and IC90s for
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47

Kondaparla, Srinivasarao, Awakash Soni, Ashan Manhas, Kumkum Srivastava, Sunil K. Puri, and S. B. Katti. "Synthesis and antimalarial activity of new 4-aminoquinolines active against drug resistant strains." RSC Advances 6, no. 107 (2016): 105676–89. http://dx.doi.org/10.1039/c6ra14016e.

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In the present study we have synthesized a new class of 4-aminoquinoline derivatives and bioevaluated them for antimalarial activity against theP. falciparum in vitro(3D7 &amp; K1) andP. yoelii in vivo(N-67 strain).
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48

Sowunmi, A., A. G. Falade, A. A. Adedeji, and C. O. Falade. "Comparative clinical characteristics and responses to oral 4-aminoquinoline therapy of malarious children who did and did not develop 4-aminoquinoline-induced pruritus." Annals of Tropical Medicine And Parasitology 95, no. 7 (2001): 645–53. http://dx.doi.org/10.1080/00034980120103216.

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49

Sowunmi, A., A. G. Falade, A. A. Adedeji, and C. O. Falade. "Comparative clinical characteristics and responses to oral 4-aminoquinoline therapy of malarious children who did and did not develop 4-aminoquinoline-induced pruritus." Annals of Tropical Medicine & Parasitology 95, no. 7 (2001): 645–53. http://dx.doi.org/10.1080/00034983.2001.11813681.

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50

Ou, Yu Heng, and Chia Ming Chang. "A Quantitative Structure-Activity Relationship Study on the Antimalarial Activities of 4-Aminoquinoline, Febrifugine and Artemisinin Compounds." International Journal of Quantitative Structure-Property Relationships 5, no. 1 (2020): 63–79. http://dx.doi.org/10.4018/ijqspr.2020010104.

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Abstract:
Quantum chemical molecular descriptors representing different types of chemical reactivity were employed to investigate the antimalarial activities of 4-aminoquinoline, febrifugine, artemisinin and their derivatives. The quantitative structure-activity relationship results reveal that: (i) the antimalarial activities of 4-aminoquinoline compounds against the chloroquine-sensitive Plasmodium falciparum 3D7 strain are mainly affected by the electron flow and polarization interactions; (ii) The reactivity descriptors for the activities of febrifugine compounds against the chloroquine-resistant Pl
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