TY - JOUR T1 - THE STRUCTURE-ACTION RELATIONSHIP OF URETHANE TYPE CHOLINESTERASE INHIBITORS JF - Journal of Pharmacology and Experimental Therapeutics JO - J Pharmacol Exp Ther SP - 457 LP - 464 VL - 122 IS - 4 AU - Francis F. Foldes AU - Gertrude Van Hees AU - David L. Davis AU - Sydney P. Shanor Y1 - 1958/04/01 UR - http://jpet.aspetjournals.org/content/122/4/457.abstract N2 - 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. ER -