The design, synthesis and physical chemical properties of novel human vasopressin V-2-receptor antagonists optimized for parenteral delivery

Authors
Ashwell, MA Bagli, JF Caggiano, TJ Chan, PS Molinari, AJ Palka, C Park, CH Rogers, JF Sherman, M Trybulski, EJ Williams, DK
Citation
Ma. Ashwell et al., The design, synthesis and physical chemical properties of novel human vasopressin V-2-receptor antagonists optimized for parenteral delivery, BIOORG MED, 10(8), 2000, pp. 783-786
Citations number
12
Categorie Soggetti
Chemistry & Analysis
Journal title
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
ISSN journal
0960894X → ACNP
Volume
10
Issue
8
Year of publication
2000
Pages
783 - 786
Database
ISI
SICI code
0960-894X(20000417)10:8<783:TDSAPC>2.0.ZU;2-J
Abstract
Ionizable groups were introduced onto the 10,11 -dihydro-5H-pyrrolo[2,1-c][ 1,4]benzodiazepine scaffold of the vasopressin V-2-antagonist WAY-VPA-985 i n the search for molecules optimized for parenteral formulation. The synthe sis and structure-activity relationships (SAR) are presented together with solubility data in a model parenteral system. The amine, WAY-140288 (4f), w as chosen for further development. (C) 2000 Elsevier Science Ltd. All right s reserved.