Synthesis and biological activity of 17-azasteroidal neuromuscular-blocking agents

AK Verma, CY Lee, S. Habtemariam, AL Harvey, DP Jindal

Research output: Contribution to journalArticle

16 Citations (Scopus)

Abstract

The new analogues, containing nitrogen at the 17-position instead of the 17a-position, of chandonium iodide 2 have been prepared and evaluated for potential neuromuscular-blocking activity in in vitro studies using chick-biventer cervicis preparations. There is a slight increase in the interonium distance between the 2 quaternary heads of 13(DPJ-240). All the bisquaternary compounds 13 (DPJ-240), 14 (DPJ-252), 15 (DPJ-262), 16 (DPJ-260) and 17 (DPJ-261) showed potent neuromuscular-blocking activity but slightly less than chandonium iodide 2. Monoquaternary ammonium derivatives 12 (DPJ-246), 21 (DPJ-245), 23 (DPJ-246) and 24 (DPJ-243) of 17-azasteroids were also synthesized and pharmacologically tested. They exhibited weak neuromuscular-blocking activity as compared to the bisquaternary compounds and chandonium iodide 2.

Original languageEnglish
Pages (from-to)331-338
Number of pages8
JournalEuropean Journal of Medicinal Chemistry
Volume29
Issue number5
DOIs
Publication statusPublished - 1 Jan 1994

Keywords

  • acetylcholine
  • bisquaternary 17-azasteroid
  • carbachol
  • chick biventer
  • monoquaternary 17-azasteroid
  • neuromuscular-blocking activity
  • neuromuscular blocking agent
  • drug synthesis

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