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 |
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Authors: | Costantino G Maltoni K Marinozzi M Camaioni E Prezeau L Pin J P Pellicciari R |
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Institution: | Dipartimento di Chimica e Tecnologia del Farmaco, Università di Perugia, Italy. |
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Abstract: | The design and synthesis of 2-(3'-(1H-tetrazol-5-yl)bicyclo1.1.1]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 microM), 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. |
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