PMID- 21924608
OWN - NLM
STAT- MEDLINE
DCOM- 20120131
LR  - 20131121
IS  - 1464-3405 (Electronic)
IS  - 0960-894X (Linking)
VI  - 21
IP  - 21
DP  - 2011 Nov 1
TI  - Discovery of spiropiperidine-based potent and selective Orexin-2 receptor 
      antagonists.
PG  - 6409-13
LID - 10.1016/j.bmcl.2011.08.094 [doi]
AB  - To generate novel human Orexin-2 Receptor (OX2R) antagonists, a spiropiperidine 
      based scaffold was designed and a SAR study was carried out. Compound 4f 
      possessed the highest OX2R antagonistic activity with an IC(50) value of 3nM with 
      450-fold selectivity against Orexin-1 Receptor (OX1R).
CI  - Copyright (c) 2011 Elsevier Ltd. All rights reserved.
FAU - Fujimoto, Tatsuhiko
AU  - Fujimoto T
AD  - Medicinal Chemistry Research Laboratories,Takeda Pharmaceutical Company, 26-1, 
      Muraokahigashi 2-Chome, Fujisawa, Kanagawa 251-1238, Japan. 
      Fujimoto_Tatsuhiko@takeda.co.jp
FAU - Tomata, Yoshihide
AU  - Tomata Y
FAU - Kunitomo, Jun
AU  - Kunitomo J
FAU - Hirozane, Mariko
AU  - Hirozane M
FAU - Marui, Shogo
AU  - Marui S
LA  - eng
PT  - Journal Article
DEP - 20110830
PL  - England
TA  - Bioorg Med Chem Lett
JT  - Bioorganic & medicinal chemistry letters
JID - 9107377
RN  - 0 (HCRTR2 protein, human)
RN  - 0 (Ligands)
RN  - 0 (Orexin Receptors)
RN  - 0 (Piperidines)
RN  - 0 (Receptors, G-Protein-Coupled)
RN  - 0 (Receptors, Neuropeptide)
RN  - 67I85E138Y (piperidine)
SB  - IM
MH  - *Drug Discovery
MH  - Ligands
MH  - Orexin Receptors
MH  - Piperidines/chemistry/*pharmacology
MH  - Receptors, G-Protein-Coupled/*antagonists & inhibitors
MH  - Receptors, Neuropeptide/*antagonists & inhibitors
EDAT- 2011/09/20 06:00
MHDA- 2012/02/01 06:00
CRDT- 2011/09/20 06:00
PHST- 2011/06/30 00:00 [received]
PHST- 2011/08/22 00:00 [revised]
PHST- 2011/08/23 00:00 [accepted]
PHST- 2011/09/20 06:00 [entrez]
PHST- 2011/09/20 06:00 [pubmed]
PHST- 2012/02/01 06:00 [medline]
AID - S0960-894X(11)01193-0 [pii]
AID - 10.1016/j.bmcl.2011.08.094 [doi]
PST - ppublish
SO  - Bioorg Med Chem Lett. 2011 Nov 1;21(21):6409-13. doi: 10.1016/j.bmcl.2011.08.094. 
      Epub 2011 Aug 30.