Design and synthesis of N-alkylated saccharins as selective alpha-1a adrenergic receptor antagonists.

Abstract

Benign prostatic hyperplasia can be managed pharmacologically with alpha-1 adrenergic receptor antagonists. Agents that demonstrate selectivity for the alpha-1a receptor subtype may offer advantages in clinical applications with respect to hypotensive side effects. The N-alkylated saccharins reported here represent a new class of subtype selective alpha-1a adrenergic receptor antagonists which demonstrate potent effects on prostate function in vivo and are devoid of blood pressure side effects.

• Authors: J B Nerenberg, J M Erb, W J Thompson, H Y Lee, J P Guare, P M Munson, J M Bergman, J R Huff, T P Broten, R S Chang, T B Chen, S O'Malley, T W Schorn, A L Scott
• Journal: Bioorganic & medicinal chemistry letters (Bioorg Med Chem Lett) Vol. 8 Issue 18 Pg. 2467-72 (Sep 22 1998) ISSN: 0960-894X [Print] England
• PMID: 9873563 (Publication Type: Journal Article)

Chemical References

• ADRA1A protein, human
• Adrenergic alpha-1 Receptor Antagonists
• Adrenergic alpha-Antagonists
• Receptors, Adrenergic, alpha-1
• Sulfonamides
• Finasteride
• Terazosin
• Saccharin
• Tamsulosin
• Prazosin

Topics

• Adrenergic alpha-1 Receptor Antagonists
• Adrenergic alpha-Antagonists (chemical synthesis, pharmacology)
• Alkylation
• Animals
• Aorta (drug effects)
• CHO Cells
• Cell Line
• Cricetinae
• Dogs
• Drug Design
• Finasteride (chemistry, pharmacology)
• Humans
• In Vitro Techniques
• Male
• Models, Chemical
• Prazosin (analogs & derivatives, chemistry, pharmacology)
• Prostate (drug effects)
• Rats
• Receptors, Adrenergic, alpha-1
• Saccharin (analogs & derivatives, chemical synthesis, pharmacology)
• Structure-Activity Relationship
• Sulfonamides (chemistry, pharmacology)
• Tamsulosin