Abstract
The effect of 15 urethane type cholinesterase inhibitors on human plasma cholinesterase (PChE) and human red cell cholinesterase (RChE) was investigated.
The inhibitory effect of the 4 structurally simplest compounds (RO1-4987 RO2-9147, neostigmine and R02-0907) was greater against PChE than against RChE.
Maximum activity against both enzymes was encountered when the distance between the quaternary N (N+) and the carbonyl carbon (C=O) atoms was between 4.7 and 5.3 Å.
Besides the N+—C=O distance, steric hindrance of the C=O or the N+, as well as other structural changes, influenced anti-cholinesterase activity.
Footnotes
- Received November 9, 1957.
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