α,α-Cyclic aminoacids as useful scaffolds for the preparation of hNK2 receptor antagonists
Graphical abstract
In the search for a novel class of hNK2 antagonists, compound 1 was identified from a tripeptide library. Subsequent optimization of binding affinity and physicochemical properties afforded 43, subnanomolar hNK2 antagonist.
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Acknowledgments
The authors thank G. Righetti and V. Caciagli for assistance in the synthesis of compounds, S. Mauro for analytical assistance, R.M. Catalioto for Caco-2 cells permeability test, D. Tagliacozzi for metabolic stability assessment, and S. Meini for biotesting. This work was supported in part by MIUR, Ministero dell’Istruzione, dell’Università e della Ricerca (Grant Ref. No. 63217).
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