Steroids and Related Studies: Part 81 - Potential Azasteroidal Neuromuscular Blockers
3β-Dimethylamino-17a-methyl-17a-aza-D-homo-5α-androstane dimethiodide (HS-777) (2) and 17β-dimethylamino-3β-pyrrolidino-5-estrene dimethiodide (HS-873) (3) have been prepared as potential neuromuscular blocking agents.Aiming at the design of 19-norchandonium iodide (4), 3β-pyrrolidino-17a-aza-D-homo-5-estren-17-one (13) has been obtained. 17a-Aza-D-homo-5α-androstane-3,17-dione obtained starting from epiandrosterone, has been converted into 2.For the synthesis of 19-norazasteroids (3 and 13), 3β-pyrrolidino-5-estren-17-one (10) prepared from 4-estrene-3,17-dione is the common intermediate.The neuromuscular blocking activity of HS-777 and HS-873 in rat phrenic nerve diaphragm preparation is one-half and one-fifth of that of chandonium iodide (1).
Bhardwaj, Tilak Raj,Kapoor, Sunil,Shekhar, C. Chandra,Jindal, Dharam Paul,Singh, Harkishan
p. 209 - 212
(2007/10/02)
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