Lipophilicity biological activity

Williams, C.A. et al., A biologically active lipophilic flavonol from Tanacetum parthenium. Phytochemistry, 38, 267, 1995. 

Hansch C, Clayton JM. Lipophilic character and biological activity of drugs. II. The parabolic case. J Pharm Soc 1973 62 1-21. 

The above Hansch equations are also generally referred to as linear free energy relationships (LFER) as they are derived from the free energy concept of the drug-receptor complex. They also assume that biological activity is linearly related to the electronic and lipophilic contributions of the various substituents on the parent molecule. 

C. Hansch and W.J. Dunn III, Linear relationships between lipophilic character and biological activity of drugs. J. Pharmaceut. Sci., 61 (1972) 1-19. 

Electrochemical study of biologically active compounds at the O/W interface provides information on physiochemical properties of the compounds at the O/W interface and in the O and W phases or, in short, hydrophobicity or lipophilicity of biologically active compounds, which seems essential to understand their biological effects, including mode of action, structure-activity relationship, delivery, and others. 

Nevertheless, numerous QSARs involve other lipophilicity dependencies to model biological activity of drugs, among which Kubinyi s bilinear relationship must be quoted [338] (see Ref 109 for a review). However, the database collected by Hansch s group showed in 1993 [339] that only 15% of the biological QSARs do not imply any lipophilicity term. Hence, lipophilicity is clearly a major determinant of biological activity [340]. 

Kubinyi, H., Lipophilicity and biological activity, Arzneim.-Forsch./Drug Res. 29,1067-1080 (1979). 

Comer, J. E. A., The acid test ionization and lipophilicity of drugs influence on biological activity, Chem. Britain 30, 983-986 (1994). 

Lipophilicity is an important consideration in the design of biologically active compounds because it often controls absorption, transport, or receptor binding that is, it is a property that can enhance the bioavailability of a compound. The presence of fluorine in a substituent gives rise to enhanced lipophilicity. 

However, these elegant glycosylated nanostructures displayed only weak biological activity relative to their native glucan elicitor counterparts. Nevertheless, such glycoclusters provided unique environments for host-guest chemistry of amphi-pathic molecules owing to their lipophilic core surrounded by a hydrophilic periphery. 

Lipophilicity is an important property of molecules in relation to their biological activities. It is one of the key physiochemical parameters that determine the distribution and transport of drugs into the body and target organs. Measurements of lipophilicity, expressed as the logarithm of the... 

Hansch C and Dunn WJ (1972) Linear Relationships Between Lipophilic Character and Biological-Activity of Drugs. J Pharm Sci 61 pp 1-19. 

S. Muranishi, A. Sakai, K. Yamada, M. Murakami, K. Tanaka, Y. Kiso, Lipophilic Peptides Synthesis of Lauryol Thyrotropin-Releasing Hormone and Its Biological Activity ,... 

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