Design and synthesis of novel dihydropyridine alpha-1A antagonists

A series of analogs of SNAP 5150 containing heteroatoms at C-2 or C-6 positions is described. Herein, we report that the presence of alkyl substituted heteroatoms at the C-2(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, mu g/kg)/K-b (IUP, dogs, mu g/kg) ratio of 14.8/2.5. (C) 1999 Elsevier Science Ltd. All rights reserved.