Synthesis and Structure-Activity Relationship of Scyliorhinin I Analogues Modified in Position 3, 6, 7 and 8

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Title:Synthesis and Structure-Activity Relationship of Scyliorhinin I Analogues Modified in Position 3, 6, 7 and 8
Creators:
Zboinska, Jolanta
Rolka, Krzysztof
Kupryszewski, Gotfryd
Golba, Krzysztof
Imiolek, Piotr
Janas, Piotr
Herman, Zbigniew S.
Journal or Publication Title:
Collection of Czechoslovak Chemical Communications, 58, 4, pp. 918-924

Abstract

Seven analogues of scyliorhinin <i>I</i> modified in positions 3, 6, 7 and 8 were synthesized by the solid-phase method. Their agonistic activity was determined on isolated guinea pig ileum (GPI). Except for the two analogues modified in position 6, all exhibited dose-dependent activity. Analogues with Phe, D-Phe(F) in position 7 and Abu in position 8 appeared significantly more active than scyliorhinin <i>I</i> and substance P, whereas the analogue with NMeLeu in position 8 appeared to be twice as active as the native molecule, but displayed only 12% of the substance P activity. CD studies indicated that the analogues modified in position 8 behaved differently in the surroundings that mimics the biological membranes.

Title:Synthesis and Structure-Activity Relationship of Scyliorhinin I Analogues Modified in Position 3, 6, 7 and 8
Creators:
Zboinska, Jolanta
Rolka, Krzysztof
Kupryszewski, Gotfryd
Golba, Krzysztof
Imiolek, Piotr
Janas, Piotr
Herman, Zbigniew S.
Divisions:Life and Chemical Sciences > Institute of Organic Chemistry and Biochemistry > Collection of Czechoslovak Chemical Communications
Journal or Publication Title:Collection of Czechoslovak Chemical Communications
Volume:58
Number:4
Page Range:pp. 918-924
ISSN:0010-0765
E-ISSN:1212-6950
Publisher:Institute of Organic Chemistry and Biochemistry
Related URLs:
URLURL Type
http://dx.doi.org/10.1135/cccc19930918UNSPECIFIED
ID Code:209
Item Type:Article
Deposited On:06 Feb 2009 16:59
Last Modified:06 Feb 2009 15:59

Citation

Zboinska, Jolanta; Rolka, Krzysztof; Kupryszewski, Gotfryd; Golba, Krzysztof; Imiolek, Piotr; Janas, Piotr; Herman, Zbigniew S. (1993) Synthesis and Structure-Activity Relationship of Scyliorhinin I Analogues Modified in Position 3, 6, 7 and 8. Collection of Czechoslovak Chemical Communications, 58 (4). pp. 918-924. ISSN 0010-0765

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