Synthesis and neuromuscular blocking activity of 16β-piperidinosteroidal derivatives

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

doi:10.1016/S0223-5234(00)01205-8

Synthesis and neuromuscular blocking activity of 16β-piperidinosteroidal derivatives

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

Strathclyde Institute Of Pharmacy And Biomedical Sciences

Research output: Contribution to journal › Article › peer-review

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.

Original language	English
Pages (from-to)	195-202
Number of pages	8
Journal	European Journal of Medicinal Chemistry
Volume	36
Issue number	2
DOIs	https://doi.org/10.1016/S0223-5234(00)01205-8
Publication status	Published - Feb 2001

Keywords

monoquaternary
bisquaternary
piperidine
chick biventer
anaesthetized cat
carbachol
nondepolarizing
steroidal

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10.1016/S0223-5234(00)01205-8

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title = "Synthesis and neuromuscular blocking activity of 16β-piperidinosteroidal derivatives",

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.",

keywords = "monoquaternary, bisquaternary, piperidine, chick biventer, anaesthetized cat, carbachol, nondepolarizing, steroidal",

author = "D.P. Jindal and P. Piplani and H. Fajrak and C.B. Prior and I.G. Marshall",

year = "2001",

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doi = "10.1016/S0223-5234(00)01205-8",

language = "English",

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journal = "European Journal of Medicinal Chemistry",

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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.

PY - 2001/2

Y1 - 2001/2

N2 - 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.

AB - 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.

KW - monoquaternary

KW - bisquaternary

KW - piperidine

KW - chick biventer

KW - anaesthetized cat

KW - carbachol

KW - nondepolarizing

KW - steroidal

U2 - 10.1016/S0223-5234(00)01205-8

DO - 10.1016/S0223-5234(00)01205-8

M3 - Article

SN - 0223-5234

VL - 36

SP - 195

EP - 202

JO - European Journal of Medicinal Chemistry

JF - European Journal of Medicinal Chemistry

IS - 2

ER -

Synthesis and neuromuscular blocking activity of 16β-piperidinosteroidal derivatives

Abstract

Keywords

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