Synthesis and Biological Evaluation of the 1-Arylpyrazole Class of σ1 Receptor Antagonists: Identification of 4-{2-[5-Methyl-1-(naphthalen-2-yl)-1H-pyrazol-3-yloxy]ethyl}morpholine (S1RA, E-52862)

José Luis Díaz; Rosa Cuberes; Joana Berrocal; Montserrat Contijoch; Ute Christmann; Ariadna Fernández; Adriana Port; Jörg Holenz; Helmut Buschmann; Christian Laggner; Maria Teresa Serafini; Javier Burgueño; Daniel Zamanillo; Manuel Merlos; José Miguel Vela; Carmen Almansa

doi:10.1021/jm3007323

Synthesis and Biological Evaluation of the 1-Arylpyrazole Class of σ1 Receptor Antagonists: Identification of 4-{2-[5-Methyl-1-(naphthalen-2-yl)-1H-pyrazol-3-yloxy]ethyl}morpholine (S1RA, E-52862)

Journal of Medicinal Chemistry ◽

10.1021/jm3007323 ◽

2012 ◽

Vol 55 (19) ◽

pp. 8211-8224 ◽

Cited By ~ 82

Author(s):

José Luis Díaz ◽

Rosa Cuberes ◽

Joana Berrocal ◽

Montserrat Contijoch ◽

Ute Christmann ◽

...

Keyword(s):

Biological Evaluation ◽

Receptor Antagonists ◽

Σ1 Receptor ◽

Synthesis And Biological Evaluation

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Synthesis and biological evaluation of novel 6,7-dihydro-5H-cyclopenta[d]pyrimidine and 5,6,7,8-tetrahydroquinazoline derivatives as sigma-1 (σ1) receptor antagonists for the treatment of pain

Bioorganic & Medicinal Chemistry Letters ◽

10.1016/j.bmcl.2016.02.077 ◽

2016 ◽

Vol 26 (8) ◽

pp. 2051-2056 ◽

Cited By ~ 4

Author(s):

Yu Lan ◽

Yiyan Songyang ◽

Lingli Zhang ◽

Yan Peng ◽

Jinchun Song

Keyword(s):

Biological Evaluation ◽

Receptor Antagonists ◽

Σ1 Receptor ◽

Sigma 1 ◽

Synthesis And Biological Evaluation

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N-(2,7-Dimethyl-2-alkyl-2H-chromen-6-yl)sulfonamide derivatives as selective serotonin 5-HT6 receptor antagonists: design, synthesis, and biological evaluation

Journal of Molecular Structure ◽

10.1016/j.molstruc.2021.131417 ◽

2021 ◽

pp. 131417

Author(s):

Aizhan Abdildinova ◽

Young Chang Kim ◽

Gee-Hyung Lee ◽

Woo-Kyu Park ◽

Heeyeong Cho ◽

...

Keyword(s):

Biological Evaluation ◽

Selective Serotonin ◽

Receptor Antagonists ◽

Design Synthesis ◽

Synthesis And Biological Evaluation

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Synthesis and biological evaluation of 4′-[(benzimidazole-1-yl)methyl]biphenyl-2-sulfonamide derivatives as dual angiotensin II/endothelin A receptor antagonists

Bioorganic & Medicinal Chemistry ◽

10.1016/j.bmc.2012.06.011 ◽

2012 ◽

Vol 20 (15) ◽

pp. 4661-4667 ◽

Cited By ~ 18

Author(s):

Renren Bai ◽

Zhen Wei ◽

Jie Liu ◽

Weijia Xie ◽

Hequan Yao ◽

...

Keyword(s):

Angiotensin Ii ◽

Biological Evaluation ◽

Receptor Antagonists ◽

Endothelin A Receptor ◽

Endothelin A ◽

Synthesis And Biological Evaluation

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Design, synthesis, and biological evaluation of 2-(5-methyl-1H-pyrazol-1-yl) acetamide derivatives as androgen receptor antagonists

Medicinal Chemistry Research ◽

10.1007/s00044-019-02291-y ◽

2019 ◽

Vol 28 (3) ◽

pp. 380-386

Author(s):

Junze Dong ◽

Jingya Zhang ◽

Zilu Li ◽

Solomon Asnake ◽

Daoguang Zhang ◽

...

Keyword(s):

Androgen Receptor ◽

Biological Evaluation ◽

Receptor Antagonists ◽

Design Synthesis ◽

Synthesis And Biological Evaluation ◽

Androgen Receptor Antagonists

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Synthesis and Biological Evaluation of Novel σ1 Receptor Ligands for Treating Neuropathic Pain: 6-Hydroxypyridazinones

Journal of Medicinal Chemistry ◽

10.1021/acs.jmedchem.5b01416 ◽

2016 ◽

Vol 59 (7) ◽

pp. 2942-2961 ◽

Cited By ~ 14

Author(s):

Xudong Cao ◽

Yin Chen ◽

Yifang Zhang ◽

Yu Lan ◽

Juecheng Zhang ◽

...

Keyword(s):

Neuropathic Pain ◽

Biological Evaluation ◽

Receptor Ligands ◽

Σ1 Receptor ◽

Synthesis And Biological Evaluation

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Design, synthesis, and biological evaluation of 2-(phenoxyaryl)-3-urea derivatives as novel P2Y1 receptor antagonists

European Journal of Medicinal Chemistry ◽

10.1016/j.ejmech.2018.09.014 ◽

2018 ◽

Vol 158 ◽

pp. 302-310 ◽

Cited By ~ 4

Author(s):

Jingjing Peng ◽

Lifen Zhao ◽

Lanlan Wang ◽

Hui Chen ◽

Yunguang Qiu ◽

...

Keyword(s):

Biological Evaluation ◽

P2y1 Receptor ◽

Receptor Antagonists ◽

Urea Derivatives ◽

Design Synthesis ◽

Synthesis And Biological Evaluation

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Design, synthesis and biological evaluation of N-hydroxy-aminobenzyloxyarylamide analogues as novel selective κ opioid receptor antagonists

Bioorganic & Medicinal Chemistry Letters ◽

10.1016/j.bmcl.2020.127236 ◽

2020 ◽

Vol 30 (13) ◽

pp. 127236

Author(s):

Guangchao He ◽

Qiao Song ◽

Junwei Wang ◽

Anhua Xu ◽

Kewen Peng ◽

...

Keyword(s):

Opioid Receptor ◽

Biological Evaluation ◽

Receptor Antagonists ◽

Design Synthesis ◽

Opioid Receptor Antagonists ◽

Synthesis And Biological Evaluation

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Design, synthesis and biological evaluation of novel 3-oxo-4-oxa-5α-androst-17β-amide derivatives as dual 5α-reductase inhibitors and androgen receptor antagonists

Bioorganic & Medicinal Chemistry Letters ◽

10.1016/j.bmcl.2017.05.078 ◽

2017 ◽

Vol 27 (17) ◽

pp. 4212-4217 ◽

Cited By ~ 2

Author(s):

Kejing Lao ◽

Jie Sun ◽

Chong Wang ◽

Ying Wang ◽

Qidong You ◽

...

Keyword(s):

Androgen Receptor ◽

Biological Evaluation ◽

Receptor Antagonists ◽

Design Synthesis ◽

Reductase Inhibitors ◽

Amide Derivatives ◽

Synthesis And Biological Evaluation ◽

Androgen Receptor Antagonists

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Synthesis and Biological Evaluation of Novel Pyridazinone-Based α4Integrin Receptor Antagonists

Journal of Medicinal Chemistry ◽

10.1021/jm060031q ◽

2006 ◽

Vol 49 (11) ◽

pp. 3402-3411 ◽

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Yong Gong ◽

J. Kent Barbay ◽

Alexey B. Dyatkin ◽

Tamara A. Miskowski ◽

Edward S. Kimball ◽

...

Keyword(s):

Biological Evaluation ◽

Receptor Antagonists ◽

Synthesis And Biological Evaluation

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Synthesis and biological evaluation of novel phenothiazine derivatives as non-peptide arginine vasopressin V2 receptor antagonists

Chinese Chemical Letters ◽

10.1016/j.cclet.2015.01.022 ◽

2015 ◽

Vol 26 (5) ◽

pp. 627-630 ◽

Cited By ~ 2

Author(s):

Shuang Zhi ◽

Shuai Mu ◽

Ying Liu ◽

Min Gong ◽

Ping-Bao Wang ◽

...

Keyword(s):

Arginine Vasopressin ◽

Biological Evaluation ◽

Phenothiazine Derivatives ◽

Receptor Antagonists ◽

Vasopressin V2 Receptor ◽

V2 Receptor ◽

Synthesis And Biological Evaluation

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