119260-54-7Relevant articles and documents
Steroids and Related Studies: Part 82 - Chandonium Related Azasteroidal Neuromuscular Blockers
Singh, Harkishan,Gupta, Rakesh Kumar,Bhardwaj, Tilak Raj
, p. 508 - 512 (2007/10/02)
Modelled on clinically active chandonium iodide (1) different azasteroidal neuromuscular blockers have been designed. 17β-Dimethylamino-3β-pyrrolidino-5-androstene dimethiodide (HS-854) (2), having not the 17a-aza-D-homo system but extranuclear quaternary ammonium head with nearly equivalent steric placement, and the 17β-dimethylamino-3α-pyrrolidino-5-androstene dimethiodide (HS-1046) (dimethiodide of 6) have been synthesized. 17β-Dimethylamino-3β-pyrrolidino-5α-androstane dimethiodide (HS-944) (7) is the dihydro analogue of HS-854 (2).The other modification, viz 6-hydroxymethyl-17β-dimethylamino-3β-pyrrolidino-5-androstene dimethiodide (HS-892) (13) has a sterically significant substituent at position-6 which should also alter hydrophilic-lipophilic balance.All the new bisquaternary steroids are active as neuromuscular blockers in the rat phrenic nerve diaphragm preparation.The structure-activity relationship has been discussed.