Citation
G. Costantino et al., Synthesis and biological evaluation of 2-(3 '-(1H-tetrazol-5-yl) bicyclo[1.1.1]pent-1-yl)glycine (S-TBPG), a novel mGlu1 receptor antagonist, BIO MED CH, 9(2), 2001, pp. 221-227
Citations number
16
Categorie Soggetti
Chemistry & Analysis
Journal title
BIOORGANIC & MEDICINAL CHEMISTRY
ISSN journal
09680896
→ ACNP
Volume
9
Issue
2
Year of publication
2001
Pages
221 - 227
Database
ISI
SICI code
0968-0896(200102)9:2<221:SABEO2>2.0.ZU;2-X
Abstract
The design and synthesis of 2-(3'-(1H-tetrazol-5-yl)bicyclo[1.1.1]pent-1-yl
)glycine (S-TBPG), a novel mGluR1 antagonist is reported. S-TBPG is charact
erized by the bioisosteric replacement of the distal carboxy group of 2-(3'
-carboxybicyclo [1.1.1]pent-1-yl)glycine (S-CBPG) by a tetrazolyl moiety. D
espite a moderate reduction in potency, S-TBPG is a selective mGluR1 antago
nist (69 muM), with no activity at other mCluR subtypes. The interesting bi
ological profile of S-TBPG, coupled with its peculiar chemical structure, i
s discussed in terms of the structure-activity relationship (SAR) of mGluR1
antagonists. (C) 2001 Elsevier Science Ltd. All rights reserved.