Design and Synthesis of Novel α1a Adrenoceptor-Selective Antagonists. 4. Structure−Activity Relationship in the Dihydropyrimidine Series

Autor: Wong, W. C., Sun, W., Lagu, B., Tian, D., Marzabadi, M. R., Zhang, F., Nagarathnam, D., Miao, S. W., Wetzel, J. M., Peng, J., Forray, C., Chang, R. S. L., Chen, T. B., Ransom, R., O'Malley, S., Broten, T. P., Kling, P., Vyas, K. P., Zhang, K., Gluchowski, C.
Zdroj: Journal of Medicinal Chemistry; November 18, 1999, Vol. 42 Issue: 23 p4804-4813, 10p
Abstrakt: We have previously disclosed dihydropyridines such as 1a,b as selective α1a 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 α1a 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.
Databáze: Supplemental Index