Abstract
We have previously disclosed dihydropyridines such as 1a,b as selective alpha(1a) antagonists as a potential treatment for benign prostatic hyperplasia (BPH). The propensity of dihydropyridines toward an oxidation led us to find suitable replacements of the core unit. The accompanying papers describe the structure-activity relationship (SAR) of dihydropyrimidinones 2a,b as selective alpha(1a) antagonists. We report herein the SAR of dihydropyrimidines such as 4 and highlight the similarities and differences between the dihydropyrimidine and dihydropyrimidinone series of compounds.
MeSH terms
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Administration, Oral
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Adrenergic alpha-1 Receptor Antagonists*
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Adrenergic alpha-Antagonists / chemical synthesis*
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Adrenergic alpha-Antagonists / chemistry
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Adrenergic alpha-Antagonists / metabolism
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Adrenergic alpha-Antagonists / pharmacology
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Animals
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Binding, Competitive
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Biological Availability
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Dogs
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Drug Design
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Drug Evaluation, Preclinical
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Humans
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In Vitro Techniques
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Male
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Prostate / metabolism
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Pyrimidines / chemical synthesis*
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Pyrimidines / chemistry
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Pyrimidines / metabolism
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Pyrimidines / pharmacology
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Rats
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Receptors, Adrenergic, alpha-1 / metabolism
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Recombinant Proteins / metabolism
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Stereoisomerism
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Structure-Activity Relationship
Substances
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ADRA1A protein, human
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Adrenergic alpha-1 Receptor Antagonists
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Adrenergic alpha-Antagonists
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Pyrimidines
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Receptors, Adrenergic, alpha-1
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Recombinant Proteins