Dicarbavasopressin antagonist analogs exhibit reduced in vivo agonist activity

In order to examine the role of the disulfide bond in vasopressin antagonists and in an attempt to prepare analogues with increased metabolic stability, the authors have prepared dicarba analogues, in which the disulfide bridge is replaced with two methylene groups. This structure preserves the 20-m...

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Bibliographic Details
Published in:Journal of medicinal chemistry 1988-08, Vol.31 (8), p.1487-1489
Main Authors: Moore, Michael L, Albrightson, Christine, Brickson, Bridget, Bryan, Heidemarie G, Caldwell, Nancy, Callahan, James F, Foster, Jonathan, Kinter, Lewis B, Newlander, Kenneth A
Format: Article
Language:English
Subjects:
Animals
Biological and medical sciences
Chemical Phenomena
Chemistry
Disulfides
Dogs
Humans
Kidney - drug effects
Medical sciences
Pharmacology. Drug treatments
Rats
Structure-Activity Relationship
Swine
Vasopressins - antagonists & inhibitors
Vasopressins - chemical synthesis
Vasopressins - pharmacology
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Summary:In order to examine the role of the disulfide bond in vasopressin antagonists and in an attempt to prepare analogues with increased metabolic stability, the authors have prepared dicarba analogues, in which the disulfide bridge is replaced with two methylene groups. This structure preserves the 20-membered cyclic portion of the molecule but may alter the overall ring geometry.
ISSN:0022-2623
1520-4804
DOI:10.1021/jm00403a001