Synthesis and neuromuscular blocking activity of 16beta-n-methylpiperazino steroidal derivatives

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

Research output: Contribution to journalArticle

11 Citations (Scopus)

Abstract

Steroidal quaternary ammonium compounds 12 and 13 with quaternised nitrogen at positions 3 and 16 of the steroidal nucleus in androstane series were synthesised and their neuromuscular blocking activities and ganglion blocking activities were studied using chick biventer and anaesthetised cat as the models. The bisquaternary compounds 12 and 13 have been found to be greater in potency than d-tubocurarine. Acetoxy derivative 13 has been found to be more potent than pipecuronium bromide taking d-tubocurarine as the standard compound indicating the need of acetoxy function at position 16.
LanguageEnglish
Pages901-908
Number of pages8
JournalEuropean Journal of Medicinal Chemistry
Volume37
Issue number11
DOIs
Publication statusPublished - 2002

Fingerprint

Tubocurarine
Pipecuronium
Quaternary Ammonium Compounds
Derivatives
Ganglia
Cats
Nitrogen
androstane

Keywords

  • neuromuscular blocking activity
  • steroidal derivatives

Cite this

Jindal, D.P. ; Piplani, P. ; Fajrak, H. ; Prior, C.B. ; Marshall, I.G. / Synthesis and neuromuscular blocking activity of 16beta-n-methylpiperazino steroidal derivatives. In: European Journal of Medicinal Chemistry. 2002 ; Vol. 37, No. 11. pp. 901-908.
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Synthesis and neuromuscular blocking activity of 16beta-n-methylpiperazino steroidal derivatives. / Jindal, D.P.; Piplani, P.; Fajrak, H.; Prior, C.B.; Marshall, I.G.

In: European Journal of Medicinal Chemistry, Vol. 37, No. 11, 2002, p. 901-908.

Research output: Contribution to journalArticle

TY - JOUR

T1 - Synthesis and neuromuscular blocking activity of 16beta-n-methylpiperazino steroidal derivatives

AU - Jindal, D.P.

AU - Piplani, P.

AU - Fajrak, H.

AU - Prior, C.B.

AU - Marshall, I.G.

PY - 2002

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AB - Steroidal quaternary ammonium compounds 12 and 13 with quaternised nitrogen at positions 3 and 16 of the steroidal nucleus in androstane series were synthesised and their neuromuscular blocking activities and ganglion blocking activities were studied using chick biventer and anaesthetised cat as the models. The bisquaternary compounds 12 and 13 have been found to be greater in potency than d-tubocurarine. Acetoxy derivative 13 has been found to be more potent than pipecuronium bromide taking d-tubocurarine as the standard compound indicating the need of acetoxy function at position 16.

KW - neuromuscular blocking activity

KW - steroidal derivatives

U2 - 10.1016/S0223-5234(02)01413-7

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