1. New V1a receptor antagonist. Part 1. Synthesis and SAR development of urea derivatives.
- Author
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Szántó G, Makó A, Baska F, Bozó É, Domány-Kovács K, Kurkó D, Cselenyák A, Mohácsi R, Kordás KS, and Bata I
- Subjects
- Antidiuretic Hormone Receptor Antagonists pharmacology, High-Throughput Screening Assays, Humans, Inhibitory Concentration 50, Piperazine chemistry, Protein Binding, Pyridines chemistry, Quinolines chemistry, Structure-Activity Relationship, Urea pharmacology, Antidiuretic Hormone Receptor Antagonists chemical synthesis, Receptors, Vasopressin metabolism, Social Behavior Disorders drug therapy, Urea chemical synthesis
- Abstract
Solid preclinical evidence links vasopressin to social behavior in animals, so, extensive work has been initiated to find new vasopressin V1a receptor antagonists which can improve deteriorated social behavior in humans and can treat the core symptoms of autistic behavior, as well. Our aim was to identify new chemical entities with antagonizing effects on vasopressin V1a receptors. Starting from a moderately potent HTS hit (7), we identified a molecule (49) having nanomolar binding strength and functional activity, which is in the same range as the potency of clinically tested V1a antagonists., Competing Interests: Declaration of Competing Interest The authors declare that they have no known competing financial interests or personal relationships that could have appeared to influence the work reported in this paper., (Copyright © 2020 Elsevier Ltd. All rights reserved.)
- Published
- 2020
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