Synthesis and structure–activity relationship studies of new endothelin pseudopeptide analogues containing alkyl spacers

…, M Hamdan, MR Mazzoni, F Calvani, P Rovero

Index: Galoppini, Claudia; Giusti, Laura; Macchia, Marco; Hamdan, Mahmoud; Mazzoni, Maria Rosaria; Calvani, Federico; Rovero, Paolo Farmaco, 1999 , vol. 54, # 4 p. 213 - 217

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Citation Number: 2

Abstract

We replaced the Asp18–Ile19 dipeptide of the C-terminal ET analogue Ph–Ph–CH2–O–N CH–CO–Phe–Asp–Ile–Ile–Trp–OH by alkyl spacers of various lengths to investigate the role of the aminoacidic central portion of the molecule and to define the N-terminal and C- terminal pharmacophoric regions of this analogue. The side-chains of the central dipeptide have been shown to be irrelevant for the binding of the molecule to the receptor, but the ...