2. Academic Validation
  3. The design, synthesis and physical chemical properties of novel human vasopressin V2-receptor antagonists optimized for parenteral delivery

The design, synthesis and physical chemical properties of novel human vasopressin V2-receptor antagonists optimized for parenteral delivery

  • Bioorg Med Chem Lett. 2000 Apr 17;10(8):783-6. doi: 10.1016/s0960-894x(00)00095-0.
M A Ashwell 1,  J F Bagli,  T J Caggiano,  P S Chan,  A J Molinari,  C Palka,  C H Park,  J F Rogers,  M Sherman,  E J Trybulski,  D K Williams
Affiliations

Affiliation

PMID: 10782686 DOI: 10.1016/s0960-894x(00)00095-0
Abstract

Ionizable groups were introduced onto the 10,11-dihydro-5H-pyrrolo[2,1-c][1,4]benzodiazepine scaffold of the vasopressin V2-antagonist WAY-VPA-985 in the search for molecules optimized for parenteral formulation. The synthesis and structure activity relationships (SAR) are presented together with solubility data in a model parenteral system. The amine, WAY-140288 (4f), was chosen for further development. p6

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