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

Article abstract of DOI:10.1016/S0960-894X(00)00247-X

On the basis of a pharmacophore definition 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 hmGlu(4a), while ineffective at group II receptor subtypes. In particular, derivative 13 is a full hmGlu(4a) agonist with an EC₅₀=17 μM. (C) 2000 Elsevier Science Ltd. All rights reserved.