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Influence of lipophilicity on the biological activity of cyclic pseudopeptide NK-2 receptor antagonists.

Abstract：

:A series of cyclic pseudopeptides of the formula cyclo(Leu psi[CH2NH]Xaa-Gln-Trp-Phe-beta Ala), where Xaa represents the residue of an alpha-amino acid, has been synthesized in order to establish the role of the Xaa side chain for tachykinin NK-2 receptor antagonist activity. Syntheses have been carried out in solid phase with either Fmoc or Boc strategy. The antagonist potency on NK-2 receptors in the hamster isolated trachea (HT) and the rabbit isolated pulmonary artery (RPA) bioassays increases with Xaa lipophilicity; cyclo(Leu psi[CH2NH]Cha-Gln-Trp-Phe-beta Ala) and cyclo(Leu psi[CH2NH]Asp(NHBzl)-Gln-Trp-Phe-beta Ala) resulted in being the two most active antagonists (pA2 = 9.06 and 9.26 on HT, respectively). A significant linear correlation was found between pA2 values determined in HT and RPA bioassays and capacity factors measured in reversed phase HPLC. The comparison between the biological activities of cyclic hexapeptides containing or not containing the aminomethylene moiety proved the crucial role of the pseudopeptide bond for determining high antagonist potency at the NK-2 receptor.

journal_name

J Med Chem

journal_title

Journal of medicinal chemistry

authors

Quartara L,Fabbri G,Ricci R,Patacchini R,Pestellini V,Maggi CA,Pavone V,Giachetti A,Arcamone F

doi

10.1021/jm00047a020

subject

Has Abstract

pub_date

1994-10-14 00:00:00

pages

3630-8

issue

21

eissn

0022-2623

issn

1520-4804

journal_volume

37

pub_type

杂志文章

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