Synthesis and neuromuscular blocking activity of 16β-piperidinosteroidal derivatives

D.P. Jindal, P. Piplani, H. Fajrak, C.B. Prior, I.G. Marshall

Research output: Contribution to journalArticle

19 Citations (Scopus)

Abstract

The synthesis and pharmacological profiles of some new steroidal mono- and bisquaternary ammonium derivatives have been described. The compounds featured have been conceptually derived structurally from two lead structures: pancuronium bromide 1 and chandonium iodide 2. In vitro and in vivo neuromuscular blocking studies have indicated the monoquaternary compound 15 to be less active than the bisquaternary compounds 10 and 11. The compound 11 has been found to be more active than d-tubocurarine.
LanguageEnglish
Pages195-202
Number of pages8
JournalEuropean Journal of Medicinal Chemistry
Volume36
Issue number2
DOIs
Publication statusPublished - Feb 2001

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Pancuronium
Tubocurarine
Ammonium Compounds
Thermodynamic properties
Pharmacology
Derivatives
chandonium iodide
In Vitro Techniques

Keywords

  • monoquaternary
  • bisquaternary
  • piperidine
  • chick biventer
  • anaesthetized cat
  • carbachol
  • nondepolarizing
  • steroidal

Cite this

Jindal, D.P. ; Piplani, P. ; Fajrak, H. ; Prior, C.B. ; Marshall, I.G. / Synthesis and neuromuscular blocking activity of 16β-piperidinosteroidal derivatives. In: European Journal of Medicinal Chemistry. 2001 ; Vol. 36, No. 2. pp. 195-202.
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Synthesis and neuromuscular blocking activity of 16β-piperidinosteroidal derivatives. / Jindal, D.P.; Piplani, P.; Fajrak, H.; Prior, C.B.; Marshall, I.G.

In: European Journal of Medicinal Chemistry, Vol. 36, No. 2, 02.2001, p. 195-202.

Research output: Contribution to journalArticle

TY - JOUR

T1 - Synthesis and neuromuscular blocking activity of 16β-piperidinosteroidal derivatives

AU - Jindal, D.P.

AU - Piplani, P.

AU - Fajrak, H.

AU - Prior, C.B.

AU - Marshall, I.G.

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KW - bisquaternary

KW - piperidine

KW - chick biventer

KW - anaesthetized cat

KW - carbachol

KW - nondepolarizing

KW - steroidal

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