The synthesis and pharmacological evaluation of indole congeners of the calcium entry blocker verapamil

Article abstract of DOI:10.1016/0223-5234(90)90028-2

Based on the notion of a bioisosteric relationship between catechol-(phenol-) and indole-amines, indole congeners of the calcium entry blocker verapamil were synthesized and examined as calcium entry blockers and as alpha¹-adrenoceptor antagonists in isolated tissue preparations and as antihypertensive agents in the spontaneously hypertensive rat.Indole 27 exhibited potent calcium entry blockade in vitro and displayed antihypertensive activity, albeit slightly less than verapamil.Indole 23 possessed both calcium entry blockade and potent alpha¹-adrenoceptor activity in vitro but in vivo was less active than verapamil as an antihypertensive agent.