Fm. Dean, HP, THE COMPONENT OF LOG-P CONTROLLING STRUCTURE-ACTIVITY-RELATIONSHIPS AMONGST NONSTEROIDAL ANTIINFLAMMATORY DRUGS, Journal of Pharmacy and Pharmacology, 48(3), 1996, pp. 233-239
A range of 25 drugs and other compounds selected from published source
s by strict criteria, has been used to confirm that their ability to i
nhibit the production of prostaglandin by mouse peritoneal macrophage
does not correlate with log P but with hP, the parameter composed of o
nly the hydrophobic contributions (atoms and groups composed of carbon
, hydrogen and halogens). Other heteroatoms and physical properties ca
n usually be ignored. Anti-inflammatory activity does not depend upon
pK(a) or partition phenomena unless extreme, nor does it depend primar
ily upon the structural types within the range phenols, salicylic acid
s, mefenamic acids, areneacetic and profenic acids.