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Journal of Enzyme Inhibition and Medicinal Chemistry Volume 34, 2019 - Issue 1
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Research Paper

Benzo[b]tiophen-3-ol derivatives as effective inhibitors of human monoamine oxidase: design, synthesis, and biological activity

Paolo GuglielmiDipartimento di Chimica e Tecnologie del Farmaco, Sapienza University of Rome, Rome, Italy; View further author information
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Daniela SecciDipartimento di Chimica e Tecnologie del Farmaco, Sapienza University of Rome, Rome, Italy; View further author information
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Anél PetzerPharmaceutical Chemistry, School of Pharmacy, Centre of Excellence for Pharmaceutical Sciences, North-West University, Potchefstroom, South Africa; View further author information
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Donatella BagettaDipartimento di Scienze della Salute, “Magna Graecia” University of Catanzaro, Campus Universitario “S. Venuta”, Viale Europa Loc. Germaneto, Catanzaro, Italy; ;Net4Science Academic Spin-Off, Campus Universitario “S. Venuta”, Viale Europa Loc. Germaneto, “Magna Graecia” University of Catanzaro, Catanzaro, Italy; View further author information
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Paola ChimentiDipartimento di Chimica e Tecnologie del Farmaco, Sapienza University of Rome, Rome, Italy; View further author information
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Giulia RotondiDipartimento di Chimica e Tecnologie del Farmaco, Sapienza University of Rome, Rome, Italy; View further author information
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Claudio FerranteDepartment of Pharmacy, “G. d’Annunzio” University of Chieti-Pescara, Chieti, Italy; View further author information
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Lucia RecinellaDepartment of Pharmacy, “G. d’Annunzio” University of Chieti-Pescara, Chieti, Italy; View further author information
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Sheila LeoneDepartment of Pharmacy, “G. d’Annunzio” University of Chieti-Pescara, Chieti, Italy; View further author information
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Stefano AlcaroDipartimento di Scienze della Salute, “Magna Graecia” University of Catanzaro, Campus Universitario “S. Venuta”, Viale Europa Loc. Germaneto, Catanzaro, Italy; ;Net4Science Academic Spin-Off, Campus Universitario “S. Venuta”, Viale Europa Loc. Germaneto, “Magna Graecia” University of Catanzaro, Catanzaro, Italy; ORCID Iconhttp://orcid.org/0000-0002-0437-358XView further author information
ORCID Icon,
Gokhan ZenginDepartment of Biology, Science Faculty, Selcuk University, Konya, TurkeyORCID Iconhttp://orcid.org/0000-0002-5165-6013View further author information
ORCID Icon,
Jacobus P. PetzerPharmaceutical Chemistry, School of Pharmacy, Centre of Excellence for Pharmaceutical Sciences, North-West University, Potchefstroom, South Africa; View further author information
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Francesco OrtusoDipartimento di Scienze della Salute, “Magna Graecia” University of Catanzaro, Campus Universitario “S. Venuta”, Viale Europa Loc. Germaneto, Catanzaro, Italy; ;Net4Science Academic Spin-Off, Campus Universitario “S. Venuta”, Viale Europa Loc. Germaneto, “Magna Graecia” University of Catanzaro, Catanzaro, Italy; ORCID Iconhttp://orcid.org/0000-0001-6235-8161View further author information
ORCID Icon &
Simone CarradoriDepartment of Pharmacy, “G. d’Annunzio” University of Chieti-Pescara, Chieti, Italy; Correspondence[email protected]
ORCID Iconhttp://orcid.org/0000-0002-8698-9440View further author information
ORCID Icon show all
Pages 1511-1525 | Received 04 Jul 2019, Accepted 02 Aug 2019, Published online: 19 Aug 2019

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Ahmed H. E. Hassan, Hyeon Jeong Kim, Min Sung Gee, Jong-Hyun Park, Hye Rim Jeon, Cheol Jung Lee, Yeonwoo Choi, Suyeon Moon, Danbi Lee, Jong Kil Lee, Ki Duk Park & Yong Sup Lee. (2022) Positional scanning of natural product hispidol’s ring-B: discovery of highly selective human monoamine oxidase-B inhibitor analogues downregulating neuroinflammation for management of neurodegenerative diseases. Journal of Enzyme Inhibition and Medicinal Chemistry 37:1, pages 768-780.
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Paolo Guglielmi, Simone Carradori, Ilaria D’Agostino, Cristina Campestre & Jacobus P. Petzer. (2022) An updated patent review on monoamine oxidase (MAO) inhibitors. Expert Opinion on Therapeutic Patents 32:8, pages 849-883.
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Articles from other publishers (14)

Bhawna, Sunil Kumar, Parvin Kumar & Ashwani Kumar. (2024) Correlation intensity index-index of ideality of correlation: A hyphenated target function for furtherance of MAO-B inhibitory activity assessment. Computational Biology and Chemistry 108, pages 107975.
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Yangjing Lv, Zhiyuan Zheng, Renzheng Liu, Jianan Guo, Changjun Zhang & Yuanyuan Xie. (2023) Monoamine oxidase B inhibitors based on natural privileged scaffolds: A review of systematically structural modification. International Journal of Biological Macromolecules 251, pages 126158.
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Liliana Pacureanu, Alina Bora & Luminita Crisan. (2023) New Insights on the Activity and Selectivity of MAO-B Inhibitors through In Silico Methods. International Journal of Molecular Sciences 24:11, pages 9583.
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Paolo Guglielmi, Virginia Pontecorvi & Atilla Akdemir. 2022. Flavonoids and Phenolics. Flavonoids and Phenolics 272 297 .
Bhawna, Ashwani Kumar, Meenakshi Bhatia, Archana Kapoor, Parvin Kumar & Sunil Kumar. (2022) Monoamine oxidase inhibitors: A concise review with special emphasis on structure activity relationship studies. European Journal of Medicinal Chemistry 242, pages 114655.
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Leticia M. Lazinski, Guy Royal, Maxime Robin, Marc Maresca & Romain Haudecoeur. (2022) Bioactive Aurones, Indanones, and Other Hemiindigoid Scaffolds: Medicinal Chemistry and Photopharmacology Perspectives. Journal of Medicinal Chemistry 65:19, pages 12594-12625.
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Munira Alrooqi, Sikandar Khan, Fahad A. Alhumaydhi, Saeed A. Asiri, Meshal Alshamrani, Mutaib M. Mashraqi, Ahmad Alzamami, Asma M. Alshahrani & Afaf A. Aldahish. (2022) A Therapeutic Journey of Pyridine-based Heterocyclic Compounds as Potent Anticancer Agents: A Review (From 2017 to 2021). Anti-Cancer Agents in Medicinal Chemistry 22:15, pages 2775-2787.
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Cheng Niu & Da-Ming Du. (2022) A squaramide-catalysed asymmetric cascade Michael addition/acyl transfer reaction between unsaturated benzothiophenones and α-nitroketones. Organic & Biomolecular Chemistry 20:4, pages 840-846.
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Sanjukta Muhuri & Habibur Rahaman. (2022) Recent Developments in Synthesis of Sulfur Heterocycles via Copper-Catalyzed C-S Bond Formation Reaction. Asian Journal of Organic & Medicinal Chemistry 7:2, pages 143-152.
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Nallappan Sundaravelu, Tushar Singha, Anuradha Nandy & Govindasamy Sekar. (2021) Copper-catalyzed domino synthesis of multi-substituted benzo[ b ]thiophene through radical cyclization using xanthate as a sulfur surrogate . Chemical Communications 57:37, pages 4512-4515.
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Bijo Mathew, Simone Carradori, Paolo Guglielmi, Md. Sahab Uddin & Hoon Kim. (2020) New Aspects of Monoamine Oxidase B Inhibitors: The Key Role of Halogens to Open the Golden Door. Current Medicinal Chemistry 28:2, pages 266-283.
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Muhammed Çeçen, Jong Min Oh, Zeynep Özdemir, Saliha Ebru Büyüktuncel, Mehtap Uysal, Mohamed A. Abdelgawad, Arafa Musa, Nicola Gambacorta, Orazio Nicolotti, Bijo Mathew & Hoon Kim. (2020) Design, Synthesis, and Biological Evaluation of Pyridazinones Containing the (2-Fluorophenyl) Piperazine Moiety as Selective MAO-B Inhibitors. Molecules 25:22, pages 5371.
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Paolo Guglielmi, Bijo Mathew, Daniela Secci & Simone Carradori. (2020) Chalcones: Unearthing their therapeutic possibility as monoamine oxidase B inhibitors. European Journal of Medicinal Chemistry 205, pages 112650.
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Nataša Perin, Valentina Rep, Irena Sović, Štefica Juričić, Danijel Selgrad, Marko Klobučar, Nataša Pržulj, Chhedi Lal Gupta, Noël Malod-Dognin, Sandra Kraljević Pavelić & Marijana Hranjec. (2020) Antiproliferative activity and mode of action analysis of novel amino and amido substituted phenantrene and naphtho[2,1-b]thiophene derivatives. European Journal of Medicinal Chemistry 185, pages 111833.
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