Abstract
The present work describes the discovery of novel series of (4,4-difluoro-1,2,3,4-tetrahydro-5H-1-benzazepine-5-ylidene)acetamide derivatives as arginine vasopressin (AVP) V(2) receptor agonists. By replacing the amide juncture in YM-35278 with a direct ring connection gave compound 10a, which acts as a V(2) receptor agonist. These studies provided the potent, orally active non-peptidic V(2) receptor agonists 10a and 10j.
MeSH terms
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Animals
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Antidiuretic Agents / chemical synthesis
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Antidiuretic Agents / chemistry
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Antidiuretic Agents / pharmacology
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Arginine Vasopressin / metabolism*
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Benzazepines / chemical synthesis*
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Benzazepines / chemistry
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Benzazepines / pharmacology
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CHO Cells
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Cricetinae
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Cricetulus
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Male
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Molecular Structure
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Radioligand Assay
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Rats
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Rats, Wistar
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Receptors, Vasopressin / agonists*
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Receptors, Vasopressin / metabolism
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Structure-Activity Relationship
Substances
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Antidiuretic Agents
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Benzazepines
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Receptors, Vasopressin
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Arginine Vasopressin