Synthesis and neuromuscular blocking activity of 16-(2- and 3-pyridylmethylene) dehydroepiandrosterone derivatives

Sonal Dubey; Amit K. Sharma; D. P. Jindal; Alan Harvey; Randhir Singh; S. L. Bodhankar

doi:10.1016/j.steroids.2010.01.009

Synthesis and neuromuscular blocking activity of 16-(2- and 3-pyridylmethylene) dehydroepiandrosterone derivatives

Sonal Dubey^*, Amit K. Sharma, D. P. Jindal, Alan Harvey, Randhir Singh, S. L. Bodhankar

^*Corresponding author for this work

Strathclyde Institute Of Pharmacy And Biomedical Sciences

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

8 Citations (Scopus)

Abstract

The interonium distance plays a major role in neuromuscular blocking activity of bis-quaternary ammonium compounds. In this study we tried to alter the distance between two quaternary nitrogens in some of the steroidal derivatives synthesized and evaluated them for neuromuscular blocking activity using in vivo (in chicks) and in vitro models (rectus abdominus and chick biventer cervis muscle) for their mechanism of action. All the synthesized compounds have shown to possess good depolarizing, competitive neuromuscular blocking activity, particularly the 17-acetoxy derivative and the increase in the distance between two quaternary nitrogens decreased the activity.

Original language	English
Pages (from-to)	323-329
Number of pages	7
Journal	Steroids
Volume	75
Issue number	4-5
DOIs	https://doi.org/10.1016/j.steroids.2010.01.009
Publication status	Published - 1 Apr 2010

Funding

We are also thankful to Council of Scientific and Industrial Research , New Delhi, India for the financial assistance. We highly appreciate the ex gratis supply of DHEA acetate by Cipla Ltd., Mumbai, India.

Keywords

depolarizing competitive antagonism
in vitro and in vivo models
neuromuscular blockers
quaternary ammonium compounds
intubating conditions
neuromuscular blocking agents
controlled study
drug dose comparison

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10.1016/j.steroids.2010.01.009

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title = "Synthesis and neuromuscular blocking activity of 16-(2- and 3-pyridylmethylene) dehydroepiandrosterone derivatives",

abstract = "The interonium distance plays a major role in neuromuscular blocking activity of bis-quaternary ammonium compounds. In this study we tried to alter the distance between two quaternary nitrogens in some of the steroidal derivatives synthesized and evaluated them for neuromuscular blocking activity using in vivo (in chicks) and in vitro models (rectus abdominus and chick biventer cervis muscle) for their mechanism of action. All the synthesized compounds have shown to possess good depolarizing, competitive neuromuscular blocking activity, particularly the 17-acetoxy derivative and the increase in the distance between two quaternary nitrogens decreased the activity.",

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AU - Dubey, Sonal

AU - Sharma, Amit K.

AU - Jindal, D. P.

AU - Harvey, Alan

AU - Singh, Randhir

AU - Bodhankar, S. L.

PY - 2010/4/1

Y1 - 2010/4/1

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AB - The interonium distance plays a major role in neuromuscular blocking activity of bis-quaternary ammonium compounds. In this study we tried to alter the distance between two quaternary nitrogens in some of the steroidal derivatives synthesized and evaluated them for neuromuscular blocking activity using in vivo (in chicks) and in vitro models (rectus abdominus and chick biventer cervis muscle) for their mechanism of action. All the synthesized compounds have shown to possess good depolarizing, competitive neuromuscular blocking activity, particularly the 17-acetoxy derivative and the increase in the distance between two quaternary nitrogens decreased the activity.

KW - depolarizing competitive antagonism

KW - in vitro and in vivo models

KW - neuromuscular blockers

KW - quaternary ammonium compounds

KW - intubating conditions

KW - neuromuscular blocking agents

KW - controlled study

KW - drug dose comparison

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JO - Steroids

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ER -

Synthesis and neuromuscular blocking activity of 16-(2- and 3-pyridylmethylene) dehydroepiandrosterone derivatives

Abstract

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Keywords

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