119808-30-9Relevant academic research and scientific papers
1-deamino-1(15)-carba and -dicarba analogues of endothelin-1
Hlavacek, Jan,Marcova, Renata,Budesinsky, Milos,Slaninova, Jirina
, p. 407 - 424 (2000)
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.
