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Updated: Aug 19, 2026

Facile Protocol for the Synthesis of Self-assembling Polyamine-based Peptide Amphiphiles (PPAs) and Related Biomaterials
Published on: June 25, 2018
Parallel solid-phase synthesis and characterization of new sulfonamide and carboxamide proline derivatives as
Paweł Zajdel1, Gilles Subra, Andrzej J Bojarski
1Laboratoire des Aminoacides, Peptides et Protéines (LAPP), UMR 5810, Faculté de Pharmacie, Université Montpellier I et II, 15 avenue Charles Flahault, 34060 Montpellier, France. mfzajdel@cyf-kr.edu.pl
Abstract:
A solid-phase synthesis of the 64-member library of novel sulfonamide and carboxamide proline derivatives, focused on the 5-HT7 receptor antagonist SB-258741, was described. The final compounds were obtained in good yields and high purity upon cleavage from SynPhase Lanterns, functionalized by a BAL linker. The library representatives were screened for 5-HT7, 5-HT1A and D2 receptors to explore the impact of a tertiary amine moiety, the length of an alkylene spacer and the aryl fragment on the receptor affinity. The preliminary biological results provided data for further investigation aimed at a search for 5-HT7 receptor agents, and permitted the identification of several compounds with significant 5-HT1A receptor affinity.
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