AbstractÐOn the basis of a pharmacophore de®nition of mGlu4 agonists, the two novel semi-rigid derivatives 12 and 13 were designed and synthesized. The preliminary biological evaluation demonstrated that both compounds interact with hmGlu4a, while ine ective at group II receptor subtypes. In particular, derivative 13 is a full hmGlu4a agonist with an EC50=17 mM.
Synthesis, Mplecular 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
MARINOZZI, Maura
2000
Abstract
AbstractÐOn the basis of a pharmacophore de®nition of mGlu4 agonists, the two novel semi-rigid derivatives 12 and 13 were designed and synthesized. The preliminary biological evaluation demonstrated that both compounds interact with hmGlu4a, while ine ective at group II receptor subtypes. In particular, derivative 13 is a full hmGlu4a agonist with an EC50=17 mM.File in questo prodotto:
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