Indole-phenol-bioisosterism. Synthesis and antihypertensive activity of a pyrrolo analog of labetalol

…, LG Humber, D Crosilla, G Oshiro…

Index: Asselin, Andre A.; Humber, Leslie G.; Crosilla, Danilo; Oshiro, George; Wojdan, Alexandra; et al. Journal of Medicinal Chemistry, 1986 ,  vol. 29,  # 6  p. 1009 - 1015

Full Text: HTML

Citation Number: 12

Abstract

The synthesis of 5-[hydl. oxy-2-[(l-methyl-3-phenylpropyl) amino] ethyl]-1H-indole-7- carboxide, 5, a pyrrolo analogue of labetalol, is described. Compound 5 was found to reduce blood pressure in spontaneously hypertensive rats with an EDm of 5 mg/kg PO, without causing any decrease in heart rate. Isolated tissue studies with 5 shows that it is a nonselective 8-adrenoceptor antagonist and that it is a weaker a-adrenoceptor antagonist ...