Tag Archives: Novartis

Reducing bioactivation potential by chemical design

Continuing the theme of an earlier post, an excellent article in Current Topics in Medicinal Chemistry looks at the issue of adverse drug events associated with the formation of reactive intermediates.  The authors (from Novartis) give some background to drug-related … Continue reading

Posted in Med Chem Strategy, Reviews, Software, Toxicology | Tagged , , , , , , , , , , , | 1 Comment

Structure-based design of BACE inhibitors

In a recent post the difficulties of developing drug-like and CNS penetrant inhibitors of β-secretase (BACE-1 or ASP-2) were hinted at (a detailed account of the state of the art can be found in this book).  Many of the reported inhibitors … Continue reading

Posted in Computational Methods, Enzyme Inhibitors, Med Chem Strategy | Tagged , , , , , , , , , , , , , , | 1 Comment

Structural Alert: Benzimidazoles

An informative letter, just published by a team from Novartis, highlights the risk of suitably substituted benzimidazoles acting as latent precursors to reactive ortho-iminoquinone species.  The example they report (see structure on left below) was Ames positive and exhibited time-dependent inhibition … Continue reading

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