Article Dans Une Revue Journal of Labelled Compounds and Radiopharmaceuticals Année : 2004

Synthesis and separation of tritiated inhibitors of aminopeptidase A and their prodrugs

Pascale Coric
Hélène Dhotel
Catherine Llorens-Cortes
  • Fonction : Auteur
Bernard Roques
  • Fonction : Auteur

Résumé

Abstract With the aim of studying the bioavailability of two related aminopeptidase A (APA) inhibitors, we have synthesized tritiated disulfide prodrugs. These molecules, 4,4′‐dithiobis‐(3,3′‐amino)‐1,1′‐butanesulfonic acid (RB 150) and its 2,2‐dimethylpropyl ester(RB 151) bearing one tritium atom per monomer in position 2 were obtained with high purity and a final specific activity of about 30 Ci/mmol. The active radiolabeled inhibitor EC 33, Ki=270 nM for APA was obtained by reduction of the disulfide bond of RB 150. Copyright © 2004 John Wiley & Sons, Ltd.

Dates et versions

hal-05115325 , version 1 (16-06-2025)

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Citer

Nicolas Inguimbert, Pascale Coric, Hélène Dhotel, Catherine Llorens-Cortes, Marie‐claude Fournié-Zaluski, et al.. Synthesis and separation of tritiated inhibitors of aminopeptidase A and their prodrugs. Journal of Labelled Compounds and Radiopharmaceuticals, 2004, 47 (13), pp.997-1005. ⟨10.1002/jlcr.888⟩. ⟨hal-05115325⟩
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