Synthesis and biological activity of conformationally controlled 2-PAM derivatives.
A series of conformationally controlled 2-PAM derivatives were prepared from 2-acetylpyridine and 2,3-pyrido[b]cycloalkenones in two steps and their reactivities towards parathion poisoned AChE were evaluated. The most planar 2,3-pyrido[b]cyclohexanone oxime methiodide showed an activity comparable to 2-PAM implying E-syn is that the most active conformation of 2-PAM in the biological system.
Jahng
Y
Y
College of Pharmacy, Yeungnam University, Kyongsan, Korea. ydjahng@ynucc.yeungnam.ac.kr
Park
J G
JG
Yoo
J W
JW
Kim
S Y
SY
Kim
T
T
Yang
J H
JH
D000110:Acetylcholinesterase / Q000378:metabolism; D001665:Binding Sites; D002801:Cholinesterase Reactivators / Q000737:chemistry*; D011220:Pralidoxime Compounds / Q000737:chemistry*; D013329:Structure-Activity Relationship
D002801:Cholinesterase Reactivators; D011220:Pralidoxime Compounds; D000110:Acetylcholinesterase; C028797:pralidoxime