hP, the component of log P controlling structure-activity relationships amongst non-steroidal anti-inflammatory drugs.
A range of 25 drugs and other compounds selected from published sources by strict criteria, has been used to confirm that their ability to inhibit the production of prostaglandin by mouse peritoneal macrophage does not correlate with log P but with hP, the parameter composed of only the hydrophobic contributions (atoms and groups composed of carbon, hydrogen and halogens). Other heteroatoms and physical properties can usually be ignored. Anti-inflammatory activity does not depend upon pKa or partition phenomena unless extreme, nor does it depend primarily upon the structural types within the range phenols, salicylic acids, mefenamic acids, areneacetic and profenic acids.
Dean
F M
FM
Department of Chemistry, University of Liverpool, UK.
D000818:Animals; D000894:Anti-Inflammatory Agents, Non-Steroidal / Q000737:chemistry* / Q000494:pharmacology*; D016861:Cyclooxygenase Inhibitors / Q000737:chemistry / Q000494:pharmacology; D017737:Macrophages, Peritoneal / Q000187:drug effects* / Q000378:metabolism; D051379:Mice; D012044:Regression Analysis; D012995:Solubility; D013329:Structure-Activity Relationship
D000894:Anti-Inflammatory Agents, Non-Steroidal; D016861:Cyclooxygenase Inhibitors