1-Deamino-1(15)-carba and -Dicarba Analogues of Endothelin-1

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Title:1-Deamino-1(15)-carba and -Dicarba Analogues of Endothelin-1
Creators:
Hlaváček, Jan
Marcová, Renáta
Buděšínský, Miloš
Slaninová, Jiřina
Journal or Publication Title:
Collection of Czechoslovak Chemical Communications, 65, 3, pp. 407-424
Uncontrolled Keywords:Peptides, Solid phase synthesis, Fragment condensation, Uterotonic activity, Disulfide isosters, Endothelin, Step-wise procedure

Abstract

Sulfanyl-methylene and ethylene bridges were inserted into the molecule of endothelin-1 (ET-1) as other possible isosteric replacements of its outer disulfide linkage. The [1-deamino-1-carba]ET-1, [1-deamino-15-carba]ET-1 and [1-deamino-1,15-dicarba]ET-1 were synthesized either by a fragment condensation of protected cyclic pentadecapeptides with carboxy-terminal hexapeptides of the endothelin-1 sequence or by step-wise coupling on polymer support of the entire henicosapeptide sequences from carboxy-terminus. The analogues were devoid of uterotonic activity in comparison with the parent ET-1. <p>

Title:1-Deamino-1(15)-carba and -Dicarba Analogues of Endothelin-1
Creators:
Hlaváček, Jan
Marcová, Renáta
Buděšínský, Miloš
Slaninová, Jiřina
Uncontrolled Keywords:Peptides, Solid phase synthesis, Fragment condensation, Uterotonic activity, Disulfide isosters, Endothelin, Step-wise procedure
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:65
Number:3
Page Range:pp. 407-424
ISSN:0010-0765
E-ISSN:1212-6950
Publisher:Institute of Organic Chemistry and Biochemistry
Related URLs:
URLURL Type
http://dx.doi.org/10.1135/cccc20000407UNSPECIFIED
ID Code:1651
Item Type:Article
Deposited On:06 Feb 2009 17:11
Last Modified:06 Feb 2009 16:11

Citation

Hlaváček, Jan; Marcová, Renáta; Buděšínský, Miloš; Slaninová, Jiřina (2000) 1-Deamino-1(15)-carba and -Dicarba Analogues of Endothelin-1. Collection of Czechoslovak Chemical Communications, 65 (3). pp. 407-424. ISSN 0010-0765

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