- Insertion of 2-carboxysuccinate and tricarballylic acid fragments into cyclic-pseudopeptides: new antagonists for the human tachykinin NK-2 receptor.
Insertion of 2-carboxysuccinate and tricarballylic acid fragments into cyclic-pseudopeptides: new antagonists for the human tachykinin NK-2 receptor.
Bioorganic & medicinal chemistry letters (2002-02-15)
Nicholas J S Harmat, Danilo Giannotti, Rossano Nannicini, Enzo Perrotta, Marco Criscuoli, Riccardo Patacchini, Anna-Rita Renzetti, Sandro Giuliani, Maria Altamura, Carlo A Maggi
PMID11844703
RESUMEN
A series of cyclic pseudopeptides were synthesized containing the sequence -Trp-Phe-(D)-PhePsiCH2NH-, the terminal ends of which were bound to 2-carboxy succinate or enantiomerically enriched tricarballylic acid to give the final cyclic structures. These two molecules and their subsequent derivatives were screened for h-NK2 receptor binding and functional antagonist activity on the rabbit urinary bladder.
MATERIALES