Synthesis and neuromuscular blocking activity of 16-(2- and 3-pyridylmethylene) dehydroepiandrosterone derivatives.
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.
Dubey
Sonal
S
KLE Academy of Higher Education and Research, College of Pharmacy, II-Block Rajajinagar, Bangalore 560010, Karnataka, India. drsonaldubey@gmail.com <drsonaldubey@gmail.com>
Sharma
Amit K
AK
Jindal
D P
DP
Harvey
Alan
A
Singh
Randhir
R
Bodhankar
S L
SL
D000818:Animals; D001001:Anura; D002645:Chickens; D003687:Dehydroepiandrosterone / Q000031:analogs & derivatives* / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology*; D018482:Muscle, Skeletal / Q000187:drug effects; D009466:Neuromuscular Blocking Agents / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology*; D012015:Reference Standards; D013997:Time Factors
D009466:Neuromuscular Blocking Agents; D003687:Dehydroepiandrosterone