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Design of Novel Bicyclic Analogues Derived from a Potent Oxytocin Antagonist by George Flouret; Olivier Chaloin; Lenka Borovickova; Jirina Slaninová is a Biochemistry, Genetics and Molecular Biology article available to read on EtoBox.

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## Abstract Eleven new analogues were synthesized by modification of the potent oxytocin antagonist (OTA) [(S)Pmp^1^, D‐Trp^2^, Pen^6^, Arg^8^]‐Oxytocin, or PA (parent antagonist), in which (S)Pmp = β,β‐(3‐thiapentamethylene)‐β‐mercapto‐propionic acid. By internal acylation of Lys, Orn, L‐1,4‐diaminobutyric acid (Dab), L‐1,3‐diaminopropionic acid (Dap) at position 4 with the __C__‐terminal Gly of the peptide tail, we prepared cyclo‐(4–9)‐[Lys^4^, Gly^9^]‐PA (pA~2~ = 8.77 ± 0.27), 1, and cyclo‐(4–9)‐[Orn^4^, Gly^9^]‐PA (pA~2~ = 8.81 ± 0.25), 3, which are equipotent with PA (pA~2~ = 8.68 ± 0.18) in the rat uterotonic assay and cyclo‐(4–9)‐[Dab^4^, Gly^9^]‐PA, 4, cyclo‐(4–9)‐[Dap^4^, Gly^9^]‐PA, 5, and cyclo‐(4–9)‐[Pmp^1^, Lys^4^, Gly^9^]‐PA, 2, which were weaker OTAs. Neither 1 nor 3 had activity as agonists or antagonists in the antidiuretic assay. In the pressor assay, both analogues 1 and 3, with pA~2~ = 7.05 ± 0.10 and pA~2~ = 6.77 ± 0.12, respectively, are somewhat weaker antagonists than PA (pA~2~ = 7.47 ± 0.35) showing significant gain in specificity. The [desamido^9^] PA‐ethylenediamine monoamide, 6, and the dimer ([desamido^9^]‐PA)~2~ ethylenediamine diamide, 7, had lower po

Who reads Design of Novel Bicyclic Analogues Derived from a Potent Oxytocin Antagonist?

Author

George Flouret; Olivier Chaloin; Lenka Borovickova; Jirina Slaninová

Publisher

John Wiley and Sons; Wiley (John Wiley & Sons); John Wiley & Sons Inc.; Wiley (ISSN 1075-2617)

Published

2006

Language

EN

Field

Biochemistry, Genetics and Molecular Biology (Life Sciences)