Synthesis, molecular modeling and preliminary biological evaluation of 1-amino-3-phosphono-3-cyclopentene-1-carboxylic acid and 1-amino-3-phosphono-2-cyclopentene-1-carboxylic acid, two novel agonists of metabotropic glutamate receptors of group III

被引：36

作者：

Amori, L

Costantino, G

Marinozzi, M

Pellicciari, R ^{[1
]}

Gasparini, F

Flor, PJ

Kuhn, R

Vranesic, I

机构：

[1] Univ Perugia, Dipartimento Chim & Tecnol Farm, I-06100 Perugia, Italy

[2] Novartis Pharma AG, Basel, Switzerland

来源：

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 2000年 / 10卷 / 13期

关键词：

D O I：

10.1016/S0960-894X(00)00247-X

中图分类号：

R914 [药物化学];

学科分类号：

100701 [药物化学];

摘要：

On the basis of a pharmacophore definition of mGlu(4) agonists, the two novel semi-rigid derivatives 12 and 13 were designed and synthesized. The preliminary biological evaluation demonstrated that both compounds interact with hmGlu(4a), while ineffective at group II receptor subtypes. In particular. derivative 13 is a full hmGlu(4a) agonist with an EC50= 17 mu M. (C) 2000 Elsevier Science Ltd. All rights reserved.

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页码：1447 / 1450

页数：4

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