title: Synthesis and biological properties of the seven alanine-modified analogues of the marine cyclopeptide hymenamide C.
abstract: The synthesis and biological activity of the marine cyclopeptide hymenamide C(1), showing an inhibitory effect on human neutrophil elastase degranulation release, were recently described. Based on this result, it was decided to undertake a systematic structure-activity relationship study of this cyclopeptide, based on the Ala-scan technique, in order to obtain useful information for the rational design of additional analogues. The synthesis and characterization of the seven Ala modified analogues are reported and their biological and pharmacological properties are described.
authors.affiliation: Dipartimento di Scienze Farmaceutiche, Università di Salerno, Fisciano, Italy.
authors.forename: Assunta
authors.initials: A
authors.lastname: Napolitano
authors.forename: Ines
authors.initials: I
authors.lastname: Bruno
authors.forename: Paolo
authors.initials: P
authors.lastname: Rovero
authors.forename: Rut
authors.initials: R
authors.lastname: Lucas
authors.forename: Miguel Payà
authors.initials: MP
authors.lastname: Peris
authors.forename: Luigi
authors.initials: L
authors.lastname: Gomez-Paloma
authors.forename: Raffaele
authors.initials: R
authors.lastname: Riccio
mesh_terms: D019943:Amino Acid Substitution; D000818:Animals; D002460:Cell Line; D015195:Drug Design; D006801:Humans; D066298:In Vitro Techniques; D051379:Mice; D009504:Neutrophils / Q000187:drug effects / Q000201:enzymology; D010456:Peptides, Cyclic / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology*; D011161:Porifera / Q000737:chemistry; D015843:Serpins / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology
chemical_list: D010456:Peptides, Cyclic; D015843:Serpins