Original scientific paper

Lipophilicity Parameters and Biological Activity in a Series of Compounds with Potential Cardiovascular Applications

Emil Pop ; Alchem Laboratories Corporation, 13305 Rachael Boulevard, Alachua, Florida 32615, USA
Daniela C. Oniciu ; Esperion Therapeutics, Inc., 3621 South State Street, 695 KMS Place, Ann Arbor, Michigan 48108, USA
Michael E. Pape ; Esperion Therapeutics, Inc., 3621 South State Street, 695 KMS Place, Ann Arbor, Michigan 48108, USA
Clay T. Cramer ; Esperion Therapeutics, Inc., 3621 South State Street, 695 KMS Place, Ann Arbor, Michigan 48108, USA
Jean-Louis H. Dasseux ; Esperion Therapeutics, Inc., 3621 South State Street, 695 KMS Place, Ann Arbor, Michigan 48108, USA

Abstract

The biological activity of some long hydrocarbon keto-diols (and their phosphate esters) and acids, has been correlated with their lipohilicity. IC₅₀ values of the hepatocyte lipid synthesis inhibition (in vitro) were used to measure biological activity; lipohilicities were calculated by employing a 3D molecular size approach implemented in a QLogP software package. Although no quantitative correlation was observed, the results of the study might be significant for in vivo application of these compounds as potential cardiovascular agents.

Keywords

cardiovascular agents; lipophilicity; log P

Hrčak ID:

102718

URI

https://hrcak.srce.hr/102718

Publication date:

31.5.2004.

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