Review in Quantitative Structure Activity Relationships on Lipoxygenase Inhibitors

Authors: Eleni P.; Dimitra H-L.

Source: Mini Reviews in Medicinal Chemistry, Volume 3, Number 5, August 2003 , pp. 487-499(13)

Publisher: Bentham Science Publishers

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Abstract:

This paper reviews and evaluates all the published QSAR treatments of LOX inhibitors. This reveals that in almost all cases, the clog P parameter plays an important part in the QSAR relationships. In some cases the steric factors (B1, B5 and L) as well as the overall molar refractivity (CMR) or the substitutents molar refractivity (MR) are important. Electronic effects except for the Hammet's constant thetas, are comparatively unimportant. The study shows that log P as calculated from the Clog P program is suitable for this form of QSAR study. Log Po of 2.77-3.76 was found to be ideal, for the biological response.

Keywords: qsar; lox inhibitors; lipophilicity; steric factors; electronic effects

Document Type: Review article

DOI: http://dx.doi.org/10.2174/1389557033487999

Affiliations: 1: Department of Pharmaceutical Chemistry, School of Pharmacy, Aristotelian University of Thessaloniki, Thessaloniki, 54124, Greece.

Publication date: 2003-08-01

More about this publication?
  • The aim of Mini-Reviews in Medicinal Chemistry is to publish short reviews on the important recent developments in medicinal chemistry and allied disciplines.

    The scope of Mini-Reviews in Medicinal Chemistry will cover all areas of medicinal chemistry including developments in rational drug design, synthetic chemistry, bioorganic chemistry, high-throughput screening, combinatorial chemistry, drug targets, and natural product research and structure-activity relationship studies.

    Mini-Reviews in Medicinal Chemistry is an essential journal for every medicinal and pharmaceutical chemist who wishes to be kept informed and up-to-date with the latest and most important developments.
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