Two novel 3′-substituted carboxycylopropylglycines, (2S,1′S,2′S,3′R)-2-(3′-xanthenylmethyl-2′-carboxycyclopropyl)glycine (8a) and (2S,1′S,2′S,3′R)-2-(3′-xanthenylethyl-2′-carboxycyclopropyl)glycine (8b), were synthesized and evaluated as mGluR ligands. Compound 8b showed to be a potent group II antagonist with submicromolar activity.
Design, Synthesis and Preliminary Evaluation of Novel 3’-Substituted Carboxycyclopropylglycines as Antagonists at Group 2 Metabotropic Glutamate Receptors / R., Pellicciari; Costantino, Gabriele; M., Marinozzi; A., Macchiarulo; Amori, Laura; P. J., Flor; F., Gasparini; R., Kuhn; S., Urwyler. - In: BIOORGANIC & MEDICINAL CHEMISTRY LETTERS. - ISSN 0960-894X. - 11:(2001), pp. 3179-3182. [10.1016/S0960-894X(01)00656-4]
Design, Synthesis and Preliminary Evaluation of Novel 3’-Substituted Carboxycyclopropylglycines as Antagonists at Group 2 Metabotropic Glutamate Receptors
COSTANTINO, Gabriele;AMORI, Laura;
2001-01-01
Abstract
Two novel 3′-substituted carboxycylopropylglycines, (2S,1′S,2′S,3′R)-2-(3′-xanthenylmethyl-2′-carboxycyclopropyl)glycine (8a) and (2S,1′S,2′S,3′R)-2-(3′-xanthenylethyl-2′-carboxycyclopropyl)glycine (8b), were synthesized and evaluated as mGluR ligands. Compound 8b showed to be a potent group II antagonist with submicromolar activity.| File | Dimensione | Formato | |
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