156329-62-3Relevant articles and documents
Quinuclidine derivative, method for preparing same and application of quinuclidine derivative
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Paragraph 0159-0160; 0163-0164, (2017/10/13)
The invention relates to a quinuclidine derivative, a pharmaceutically acceptable salt, pro-drug and solvent compound of the quinuclidine derivative, a method for preparing the quinuclidine derivative, a drug composition with the quinuclidine derivative and the pharmaceutically acceptable salt, pro-drug and solvent compound and pharmaceutical application of the quinuclidine derivative. The quinuclidine derivative, the pharmaceutically acceptable salt, pro-drug and solvent compound, the method, the drug composition and the pharmaceutical application have the advantage that the compound is excellent in M3 receptor antagonist activity and accordingly can be used as a novel efficient drug for chronic obstructive pulmonary diseases.
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
Costantino, Gabriele,Maltoni, Katiuscia,Marinozzi, Maura,Camaioni, Emidio,Prezeau, Laurent,Pin, Jean-Philippe,Pellicciari, Roberto
, p. 221 - 227 (2007/10/03)
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 characterized 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. Despite a moderate reduction in potency, S-TBPG is a selective mGluR1 antagonist (69 μM), with no activity at other mGluR subtypes. The interesting biological profile of S-TBPG, coupled with its peculiar chemical structure, is discussed in terms of the structure-activity relationship (SAR) of mGluR1 antagonists.