Discovery and SAR of Potent, Orally Available and Brain-Penetrable 5,6-Dihydro-4H-3-thia-1-aza-benzo[e]azulen- and 4,5-Dihydro-6-oxa-3-thia-1-aza-benzo[e]azulen Derivatives as Neuropeptide Y Y5 Receptor Antagonists.

ChemInform ◽  
2004 ◽  
Vol 35 (37) ◽  
Author(s):  
Heinrich Rueeger ◽  
Marc Gerspacher ◽  
Peter Buehlmayer ◽  
Pascal Rigollier ◽  
Yasuchika Yamaguchi ◽  
...  
Keyword(s):  
Neuropeptide Y ◽  
Receptor Antagonists

Design, synthesis and evaluation of a novel cyclohexanamine class of neuropeptide Y Y1 receptor antagonists

2009 ◽  
Vol 19 (16) ◽  
pp. 4781-4785 ◽  
Author(s):  
Kaimei Cho ◽  
Makoto Ando ◽  
Kensuke Kobayashi ◽  
Hiroshi Miyazoe ◽  
Toshiaki Tsujino ◽  
...  
Keyword(s):  
Neuropeptide Y ◽  
Receptor Antagonists ◽  
Design Synthesis ◽  
Y1 Receptor

Synthesis and Evaluation of New Arylsulfonamidomethylcyclohexyl Derivatives as Human Neuropeptide Y Y5 Receptor Antagonists for the Treatment of Obesity.

ChemInform ◽  
2004 ◽  
Vol 35 (30) ◽  
Author(s):  
Antonio Moreno ◽  
Silvia Perez ◽  
Silvia Galiano ◽  
Laura Juanenea ◽  
Oihana Erviti ◽  
...  
Keyword(s):  
Neuropeptide Y ◽  
Receptor Antagonists ◽  
Treatment Of Obesity

Discovery of neuropeptide Y receptor antagonists

1997 ◽  
pp. 191-201 ◽  
Author(s):  
Alexandr Rabinovich ◽  
Anatoly Mazurov ◽  
Galina Krokhina ◽  
Anthony Ling ◽  
Nurit Livnah ◽  
...  
Keyword(s):  
Neuropeptide Y ◽  
Receptor Antagonists ◽  
Neuropeptide Y Receptor

1,3-Disubstituted benzazepines as neuropeptide Y Y1 receptor antagonists

1999 ◽  
Vol 7 (8) ◽  
pp. 1703-1714 ◽  
Author(s):  
Yasushi Murakami ◽  
Sanji Hagishita ◽  
Tetsuo Okada ◽  
Makoto Kii ◽  
Hiroshi Hashizume ◽  
...  
Keyword(s):  
Neuropeptide Y ◽  
Receptor Antagonists ◽  
Y1 Receptor

Highly Selective and Potent Neuropeptide Y (NPY) Y1 Receptor Antagonists Based on [Pro30, Tyr32, Leu34]NPY(28-36)-NH2(BW1911U90)†

2001 ◽  
Vol 44 (10) ◽  
pp. 1479-1482 ◽  
Author(s):  
Ambikaipakan Balasubramaniam ◽  
Vikas C. Dhawan ◽  
Deborra E. Mullins ◽  
William T. Chance ◽  
Sulaiman Sheriff ◽  
...  
Keyword(s):  
Neuropeptide Y ◽  
Receptor Antagonists ◽  
Y1 Receptor

Neuropeptide Y receptor antagonists in obesity

1997 ◽  
Vol 6 (12) ◽  
pp. 1827-1838 ◽  
Author(s):  
Donald R Gehlert ◽  
Philip A Hipskind
Keyword(s):  
Neuropeptide Y ◽  
Receptor Antagonists ◽  
Neuropeptide Y Receptor

Dimeric argininamide-type neuropeptide Y receptor antagonists: Chiral discrimination between Y1 and Y4 receptors

2013 ◽  
Vol 21 (21) ◽  
pp. 6303-6322 ◽  
Author(s):  
Max Keller ◽  
Melanie Kaske ◽  
Tobias Holzammer ◽  
Günther Bernhardt ◽  
Armin Buschauer
Keyword(s):  
Neuropeptide Y ◽  
Chiral Discrimination ◽  
Receptor Antagonists ◽  
Neuropeptide Y Receptor

scholarly journals Argininamide-type neuropeptide Y Y1 receptor antagonists: the nature of Nω-carbamoyl substituents determines Y1R binding mode and affinity

2020 ◽  
Vol 11 (2) ◽  
pp. 274-282
Author(s):  
Jonas Buschmann ◽  
Theresa Seiler ◽  
Günther Bernhardt ◽  
Max Keller ◽  
David Wifling
Keyword(s):  
Neuropeptide Y ◽  
Binding Mode ◽  
Reference Compound ◽  
Induced Fit Docking ◽  
Receptor Antagonists ◽  
Induced Fit ◽  
Y1 Receptor

Replacement of the carbamoyl residue (R) in reference compound 2 by larger residues (e.g.72) strongly affected Y1R affinity. In case of very bulky carbamoyl substituents (e.g.78), an inverted binding mode was suggested by induced-fit docking.

Sign in / Sign up

Export Citation Format

Share Document