Synthesis and neuromuscular blocking activity of 16beta-piperidinosteroidal derivatives.
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.
Jindal
D P
DP
University Institute of Pharmaceutical Sciences, Panjab University, 160 014, Chandigarh, India. dpjindal@USA.net
Piplani
P
P
Fajrak
H
H
Prior
C
C
Marshall
I G
IG
D000818:Animals; D001667:Binding, Competitive; D002217:Carbachol / Q000037:antagonists & inhibitors; D002415:Cats; D002645:Chickens; D018679:Cholinergic Agonists / Q000378:metabolism; D018680:Cholinergic Antagonists / Q000138:chemical synthesis / Q000494:pharmacology; D009132:Muscles / Q000187:drug effects; D009466:Neuromuscular Blocking Agents / Q000138:chemical synthesis* / Q000494:pharmacology; D013256:Steroids / Q000138:chemical synthesis / Q000494:pharmacology
D018679:Cholinergic Agonists; D018680:Cholinergic Antagonists; D009466:Neuromuscular Blocking Agents; D013256:Steroids; D002217:Carbachol