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Synthesis and neuromuscular blocking activity of 16β-piperidinosteroidal derivatives

Jindal, D.P. and Piplani, P. and Fajrak, H. and Prior, C.B. and Marshall, I.G. (2001) Synthesis and neuromuscular blocking activity of 16β-piperidinosteroidal derivatives. European Journal of Medicinal Chemistry, 36 (2). pp. 195-202. ISSN 0223-5234

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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.