2. Academic Validation
  3. Development of dual V1a/V2 antagonists containing triazolobenzazepine scaffold

Development of dual V1a/V2 antagonists containing triazolobenzazepine scaffold

  • Eur J Med Chem. 2024 Nov 28:283:117069. doi: 10.1016/j.ejmech.2024.117069.
Gábor Varró 1,  Éva Bozó 2,  Krisztina Vukics 2,  Ferenc Baska 2,  Gábor Szántó 2,  Balázs Krámos 2,  Katalin Domány-Kovács 2,  Krisztina Szondiné Kordás 2,  Mónika Vastag 2,  Ildikó Magdó 2,  Imre Bata 2
Affiliations

Affiliations

  • 1 Gedeon Richter Plc, Budapest 10, PO Box 27, H-1475, Hungary. Electronic address: varrog@gedeonrichter.com.
  • 2 Gedeon Richter Plc, Budapest 10, PO Box 27, H-1475, Hungary.
PMID: 39631099 DOI: 10.1016/j.ejmech.2024.117069
Abstract

The development of a dual V1a/V2 antagonist compound is a complex and challenging task. Conivaptan is up to now the only known V1a/V2 antagonist which was approved for the treatment of euvolemic hyponatremia. Previously, we reported RGH-122, a novel selective V1a antagonist compound. Herein, we describe several promising dual antagonist compounds, which are derived from RGH-122 by using modifications in its tail region. These modifications can result in excellent binding affinity on both V1a and V2 receptors.

Keywords

In silico docking; Triazolobenzazepine; V1a/V2 dual antagonist.

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