The world's first wiki where authorship really matters (Nature Genetics, 2008). Due credit and reputation for authors. Imagine a global collaborative knowledge base for original thoughts. Search thousands of articles and collaborate with scientists around the globe.

wikigene or wiki gene protein drug chemical gene disease author authorship tracking collaborative publishing evolutionary knowledge reputation system wiki2.0 global collaboration genes proteins drugs chemicals diseases compound
Hoffmann, R. A wiki for the life sciences where authorship matters. Nature Genetics (2008)

Pharmacokinetic screening of o-naphthoquinone 5-lipoxygenase inhibitors.

The o-naphthoquinone derivative, CGS 8515 (I), is a potent inhibitor (IC50, 0.1 microM) of 5-lipoxygenase, but its therapeutic potential is compromised by a short plasma half-life (22 min) and extremely poor oral bioavailability (less than 2%). Poor biopharmaceutical properties of CGS 8515 were attributed to poor aqueous solubility and rapid in vivo hydrolysis of its methyl ester function to an inactive metabolite (IC50, 100 microM). An active amide analogue (II) was synthesized to prevent rapid hydrolysis. While analogue II appeared to be stable in vivo, its plasma half-life was also short (10 min), possibly because of rapid tissue distribution rather than metabolic elimination. Therefore, three potent analogues with increased aqueous solubilities were synthesized and compared with respect to their pharmacokinetic properties. The analogue with the highest aqueous solubility (V) demonstrated a plasma concentration vs time profile with the largest area under the curve (AUC) and the smallest distribution (alpha) phase of all the analogues studied. The percentage AUC of the terminal phase (beta) for three analogs paralleled their aqueous solubilities. The oral bioavailability of V was improved to 27%, compared to 2% for the parent compound, CGS 8515.[1]


  1. Pharmacokinetic screening of o-naphthoquinone 5-lipoxygenase inhibitors. Rakhit, A., Kuwahara, S.K., Jones, D.R., Soliman, V.F., Kotake, A.N., Oglesby, T.D., Wasley, J.W., Tripp, S.L., Douglas, F.L. Pharm. Res. (1990) [Pubmed]
WikiGenes - Universities