Category Archives: European Journal of Medicinal Chemistry

Discovery of 1,2-diaryl-3-oxopyrazolidin-4-carboxamides as a new class of MurA enzyme inhibitors and characterization of their antibacterial activity

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Publication date: 5 December 2023

Source: European Journal of Medicinal Chemistry, Volume 261

Author(s): Reem A. Wagdy, Nader S. Abutaleb, Reem K. Fathalla, Yehia Elgammal, Stefanie Weck, Rusha Pal, Patrick D. Fischer, Christian Ducho, Ashraf H. Abadi, Mohamed N Seleem, Matthias Engel, Mohammad Abdel-Halim

Design, synthesis, and anti-respiratory syncytial virus potential of novel 3-(1,2,3-triazol-1-yl)furoxazine-fused benzimidazole derivatives

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Publication date: 5 December 2023

Source: European Journal of Medicinal Chemistry, Volume 261

Author(s): Lu Mao, Song Wang, Ying Qu, Haixia Wang, Yifan Zhao, Chuantao Zhu, Zhongmou Zhang, Chengyun Jin, Piet Herdewijn, Feng-Wu Liu, Zhenya Wang

Galantamine-memantine hybrids for Alzheimer’s disease: The influence of linker rigidity in biological activity and pharmacokinetic properties

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Publication date: 5 December 2023

Source: European Journal of Medicinal Chemistry, Volume 261

Author(s): Filippo Basagni, Jose A. Ortega, Sine M. Bertozzi, Andrea Armirotti, Maria Summa, Rosalia Bertorelli, Manuela Bartolini, Ian R. Mellor, Martina Bedeschi, Giovanni Bottegoni, Vittorio Lembo, Anna Minarini, Andrea Cavalli, Michela Rosini

Synthesis, cytotoxic activity evaluation and mechanistic investigation of novel 3,7-diarylsubstituted 6-azaindoles

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Publication date: 5 December 2023

Source: European Journal of Medicinal Chemistry, Volume 261

Author(s): Nikolaos Lougiakis, Nikolaos Sakalis, Maria Georgiou, Panagiotis Marakos, Nicole Pouli, Alexios-Leandros Skaltsounis, Eleni Mavrogonatou, Harris Pratsinis, Dimitris Kletsas

Discovery of novel multifunctional ligands targeting GABA transporters, butyrylcholinesterase, β-secretase, and amyloid β aggregation as potential treatment of Alzheimer’s disease

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Publication date: 5 December 2023

Source: European Journal of Medicinal Chemistry, Volume 261

Author(s): Paula Zaręba, Kamil Łątka, Gabriela Mazur, Beata Gryzło, Anna Pasieka, Justyna Godyń, Dawid Panek, Anna Skrzypczak-Wiercioch, Georg C. Höfner, Gniewomir Latacz, Maciej Maj, Alba Espargaró, Raimon Sabaté, Krzysztof Jóźwiak, Klaus T. Wanner, Kinga Sałat, Barbara Malawska, Katarzyna Kulig, Marek Bajda

PITB: A high affinity transthyretin aggregation inhibitor with optimal pharmacokinetic properties

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Publication date: 5 December 2023

Source: European Journal of Medicinal Chemistry, Volume 261

Author(s): Francisca Pinheiro, Nathalia Varejão, Adrià Sánchez-Morales, Filipa Bezerra, Susanna Navarro, Adrián Velázquez-Campoy, Félix Busqué, Maria Rosário Almeida, Ramon Alibés, David Reverter, Irantzu Pallarès, Salvador Ventura

Design, synthesis, and biological evaluation of novel 4,4′-bipyridine derivatives acting as CDK9-Cyclin T1 protein-protein interaction inhibitors against triple-negative breast cancer

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Publication date: 5 December 2023

Source: European Journal of Medicinal Chemistry, Volume 261

Author(s): Guiping Gao, Jiayi Li, Yin Cao, Xudan Li, Yuqing Qian, Xiumei Wang, Mengyu Li, Yingkun Qiu, Tong Wu, Liqiang Wang, Meijuan Fang

Indirubin derivatives as bifunctional molecules inducing DNA damage and targeting PARP for the treatment of cancer

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Publication date: 5 December 2023

Source: European Journal of Medicinal Chemistry, Volume 261

Author(s): Siyuan Wan, Xinye Chen, Fucheng Yin, Shang Li, Yonglei Zhang, Heng Luo, Zhongwen Luo, Ningjie Cui, Yifan Chen, Xinxin Li, Lingyi Kong, Xiaobing Wang

Exploring the structural-activity relationship of hexahydropyrazino[1,2-d]pyrido[3,2-b][1,4]oxazine derivatives as potent and orally-bioavailable PARP7 inhibitors

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Publication date: 5 December 2023

Source: European Journal of Medicinal Chemistry, Volume 261

Author(s): Silong Zhang, Yu Zhang, Ziwei Wang, Luolong Qing, Shaojuan Fu, Juan Xu, Yuanyuan Li, Huaxiang Fang, Huan He

Non-peptidic immunoproteasome β5i-selective inhibitor as potential treatment for idiopathic pulmonary fibrosis: Virtual screening, hit evolution and lead identification

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Publication date: 5 December 2023

Source: European Journal of Medicinal Chemistry, Volume 261

Author(s): Yunxuan Li, Guanglei Nan, Xianxin Hou, Yechao Yan, Yajun Yang, Ying Yang, Ke Li, Zhiyan Xiao