Scaffold hopping, synthesis and structure–activity relationships of 5,6-diaryl-pyrazine-2-amide derivatives: A novel series of CB1 receptor antagonists

Jonas Boström; Kristina Berggren; Thomas Elebring; Peter J. Greasley; Michael Wilstermann

doi:10.1016/j.bmc.2007.03.075

Scaffold hopping, synthesis and structure–activity relationships of 5,6-diaryl-pyrazine-2-amide derivatives: A novel series of CB1 receptor antagonists

Bioorganic & Medicinal Chemistry ◽

10.1016/j.bmc.2007.03.075 ◽

2007 ◽

Vol 15 (12) ◽

pp. 4077-4084 ◽

Cited By ~ 47

Author(s):

Jonas Boström ◽

Kristina Berggren ◽

Thomas Elebring ◽

Peter J. Greasley ◽

Michael Wilstermann

Keyword(s):

Cb1 Receptor ◽

Scaffold Hopping ◽

Receptor Antagonists ◽

Structure Activity Relationships ◽

Structure Activity ◽

Amide Derivatives ◽

Cb1 Receptor Antagonists

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Structure–Activity Relationships and Conformational Freedom of CB1 Receptor Antagonists and Inverse Agonists

The Cannabinoid Receptors ◽

10.1007/978-1-59745-503-9_4 ◽

2009 ◽

pp. 95-119 ◽

Cited By ~ 1

Author(s):

Yanan Zhang ◽

Herbert H. Seltzman ◽

Marcus Brackeen ◽

Brian F. Thomas

Keyword(s):

Cb1 Receptor ◽

Receptor Antagonists ◽

Inverse Agonists ◽

Structure Activity Relationships ◽

Structure Activity ◽

Conformational Freedom ◽

Cb1 Receptor Antagonists

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ChemInform Abstract: Indole Amide Derivatives: Synthesis, Structure-Activity Relationships, and Molecular Modeling Studies of a New Series of Histamine H1-Receptor Antagonists.

ChemInform ◽

10.1002/chin.199929124 ◽

2010 ◽

Vol 30 (29) ◽

pp. no-no

Author(s):

Sandra Battaglia ◽

Enrico Boldrini ◽

Federico Da Settimo ◽

Giulio Dondio ◽

Concettina La Motta ◽

...

Keyword(s):

Molecular Modeling ◽

H1 Receptor ◽

Receptor Antagonists ◽

Histamine H1 Receptor ◽

Structure Activity Relationships ◽

Structure Activity ◽

Modeling Studies ◽

Amide Derivatives ◽

Molecular Modeling Studies

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Indole amide derivatives: synthesis, structure–activity relationships and molecular modelling studies of a new series of histamine H1-receptor antagonists

European Journal of Medicinal Chemistry ◽

10.1016/s0223-5234(99)80044-0 ◽

1999 ◽

Vol 34 (2) ◽

pp. 93-105 ◽

Cited By ~ 28

Author(s):

Sandra Battaglia ◽

Enrico Boldrini ◽

Federico Da Settimo ◽

Giulio Dondio ◽

Concettina La Motta ◽

...

Keyword(s):

Molecular Modelling ◽

H1 Receptor ◽

Receptor Antagonists ◽

Histamine H1 Receptor ◽

Structure Activity Relationships ◽

Structure Activity ◽

Amide Derivatives ◽

Molecular Modelling Studies ◽

Modelling Studies

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Discovery of novel pyrazolo[1,5-a]pyridine-based EP1 receptor antagonists by scaffold hopping: Design, synthesis, and structure-activity relationships

Bioorganic & Medicinal Chemistry Letters ◽

10.1016/j.bmcl.2017.07.055 ◽

2017 ◽

Vol 27 (17) ◽

pp. 4044-4050 ◽

Cited By ~ 4

Author(s):

Yosuke Nishigaya ◽

Kentaro Umei ◽

Yoshifumi Saito ◽

Hiroyuki Watanabe ◽

Tatsuhiro Kondo ◽

...

Keyword(s):

Scaffold Hopping ◽

Receptor Antagonists ◽

Design Synthesis ◽

Structure Activity Relationships ◽

Structure Activity ◽

Ep1 Receptor

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Synthesis, Molecular Pharmacology, and Structure–Activity Relationships of 3-(Indanoyl)indoles as Selective Cannabinoid Type 2 Receptor Antagonists

Journal of Medicinal Chemistry ◽

10.1021/acs.jmedchem.1c00442 ◽

2021 ◽

Author(s):

Harvey F. Fulo ◽

Amal Shoeib ◽

Christian V. Cabanlong ◽

Alexander H. Williams ◽

Chang-Guo Zhan ◽

...

Keyword(s):

Molecular Pharmacology ◽

Receptor Antagonists ◽

Structure Activity Relationships ◽

Structure Activity

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Synthesis and Structure−Activity Relationships of 2-Substitutedd-Tryptophan-Containing Peptidic Endothelin Receptor Antagonists: Importance of the C-2 Substituent of thed-Tryptophan Residue for Endothelin A and B Receptor Subtype Selectivity

Journal of Medicinal Chemistry ◽

10.1021/jm9600914 ◽

1996 ◽

Vol 39 (12) ◽

pp. 2313-2330 ◽

Cited By ~ 14

Author(s):

Takehiro Fukami ◽

Takeru Yamakawa ◽

Kenji Niiyama ◽

Hisaki Kojima ◽

Yuuka Amano ◽

...

Keyword(s):

Tryptophan Residue ◽

Receptor Subtype ◽

Endothelin Receptor Antagonists ◽

Endothelin Receptor ◽

Receptor Antagonists ◽

Structure Activity Relationships ◽

Subtype Selectivity ◽

Structure Activity ◽

Endothelin A

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Synthesis and structure activity relationships of glycine amide derivatives as novel Vascular Adhesion Protein-1 inhibitors

Bioorganic & Medicinal Chemistry ◽

10.1016/j.bmc.2016.10.025 ◽

2017 ◽

Vol 25 (1) ◽

pp. 187-201 ◽

Cited By ~ 6

Author(s):

Susumu Yamaki ◽

Daisuke Suzuki ◽

Jiro Fujiyasu ◽

Masahiro Neya ◽

Akira Nagashima ◽

...

Keyword(s):

Adhesion Protein ◽

Structure Activity Relationships ◽

Structure Activity ◽

Amide Derivatives ◽

Vascular Adhesion ◽

Vascular Adhesion Protein 1

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Selective endothelin A receptor antagonists. 2. Discovery and structure-activity relationships of 5-ketopentanoic acid derivatives

European Journal of Medicinal Chemistry ◽

10.1016/s0223-5234(97)84014-7 ◽

1997 ◽

Vol 32 (6) ◽

pp. 515-522 ◽

Cited By ~ 8

Author(s):

P.C. Astles ◽

T.J. Brown ◽

N.V. Harris ◽

M.F. Harper ◽

C McCarthy ◽

...

Keyword(s):

Receptor Antagonists ◽

Structure Activity Relationships ◽

Structure Activity ◽

Endothelin A Receptor ◽

Endothelin A

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Synthesis and structure–activity relationships of ( R )-1-alkyl-3-[2-(2-amino)phenethyl]-5-(2-fluorophenyl)-6-methyluracils as human GnRH receptor antagonists

Bioorganic & Medicinal Chemistry Letters ◽

10.1016/j.bmcl.2004.02.004 ◽

2004 ◽

Vol 14 (9) ◽

pp. 2269-2274 ◽

Cited By ~ 14

Author(s):

Martin W Rowbottom ◽

Fabio C Tucci ◽

Yun-Fei Zhu ◽

Zhiqiang Guo ◽

Timothy D Gross ◽

...

Keyword(s):

Gnrh Receptor ◽

Receptor Antagonists ◽

Structure Activity Relationships ◽

Structure Activity

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Design of 2,5-Dimethyl-3-(6-dimethyl-4-methylpyridin-3-yl)-7-dipropylaminopyrazolo[1,5-a]pyrimidine (NBI 30775/R121919) and Structure−Activity Relationships of a Series of Potent and Orally Active Corticotropin-Releasing Factor Receptor Antagonists

Journal of Medicinal Chemistry ◽

10.1021/jm040058e ◽

2004 ◽

Vol 47 (19) ◽

pp. 4787-4798 ◽

Cited By ~ 91

Author(s):

Chen ◽

Keith M. Wilcoxen ◽

Charles Q. Huang ◽

Yun-Feng Xie ◽

James R. McCarthy ◽

...

Keyword(s):

Corticotropin Releasing Factor ◽

Receptor Antagonists ◽

Structure Activity Relationships ◽

Structure Activity ◽

Orally Active

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