Journal
BIOORGANIC & MEDICINAL CHEMISTRY
Volume 11, Issue 20, Pages 4449-4454Publisher
PERGAMON-ELSEVIER SCIENCE LTD
DOI: 10.1016/S0968-0896(03)00488-7
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For a series of monosubstituted arylguanidines, 5-HT3 receptor affinity was found generally related to the electron withdrawing nature of the substituent at the aryl 3-position and the lipophilicity of the 4-position substituent. A broader examination of 35 arylguanidines and arylbiguanides revealed that affinity could be described by molecular polarizability, a Chi index term ((8)chi(P)), and the sum of all (-Cl) E-State values (SsCl) in the molecule. (C) 2003 Elsevier Ltd. All rights reserved.
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