Gerardine Burton | Researchain

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Bioorganic & Medicinal Chemistry Letters | 2003

Dihydroquinolines with amine-containing side chains as potent n-NOS inhibitors

Stefan Jaroch; Peter Hölscher; Hartmut Rehwinkel; Detlev Sülzle; Gerardine Burton; Margrit Hillmann; Fiona Mcdougall Mcdonald

Dihydroquinolines with aminoalkyl side chains have been synthesized and have been shown to be potent n-NOS inhibitors. A marked selectivity versus e-NOS of up to approximately 300-fold was observed, whereas i-NOS was moderately inhibited.

Bioorganic & Medicinal Chemistry Letters | 2002

Dihydroquinolines as novel n-NOS inhibitors

Stefan Jaroch; Peter Hölscher; Hartmut Rehwinkel; Detlev Sülzle; Gerardine Burton; Margrit Hillmann; Fiona Mcdougall Mcdonald

Dihydroquinolines have been synthesized and have been shown to be potent n-NOS inhibitors. Selectivity versus e-NOS was increased to approximately 100-fold through appropriate substitution at the benzene ring.

Archive | 2002

Forum Discussion: ADME-Based Compound Optimization and Selection Paradigm

Andreas Baumann; Martin K. Bayliss; Thorsten Blume; Ulf Boemer; Gerardine Burton; Gabriele Cruziani; Karsten Denner; John Dixon; Nikolaus Heinrich; Thierry Lavé; Jiunn Lin; Arun Mandagere; Geert Mannens; Timothy Olah; Olavi Pelkonen; Joe Post; Iris Pribilla; Andreas Reichel; Andrea Rotgeri; Herbert Schneider; Gerd Siemeister; Dennis A. Smith; Thomas Steger-Hartmann; Babu Subramanyam; Han van de Waterbeemd; Ron Vergona; Bjorn Wallmark; Christian Wienhold

I have a few questions relating to your filtration or artificial membrane model. Could one explanation for your poor correlation with the Caco-2 data be that you use a different solvent concentration?

Archive | 1996