Design and synthesis of novel dihydropyridine alpha-1A antagonists

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• 作者：Marzabadi ; Mohammad R. ; Hong ; Xingfang ; Nagarathnam ; Dhanapalan ; Miao ; ShouWu ; Chiu ; George ; et. al.
• 刊名：Bioorganic and Medicinal Chemistry Letters
• 出版年：1999
• 出版时间：October 4, 1999
• 年：1999
• 卷：9
• 期：1
• 页码：2843-2848
• 全文大小：285 K

文摘

A series of analogs of SNAP 5150 containing heteroatoms at C₂ or C₆ positions is described. Herein, we report that the presence of alkyl substituted heteroatoms at the C₂₍₆₎-positions of the dihydropyridine are well tolerated. In addition, 15 inhibited the phenylephrine induced contraction of dog prostate tissue with a K_b of 1.5 nM and showed a K_b (DBP, dogs, μg/kg)/K_b (IUP, dogs, μg/kg) ratio of 14.8/2.5.