Tag Archives: CYP450

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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Discovery of PF-232798 (CCR5 Antagonist)


CCR5 antagonists prevent entry of HIV into host cells by binding to the CCR5 co-receptor and stopping the gp120-CD4 complex from making the crucial interaction with CCR5 that leads to fusion of the viral and host cell membranes (see Wikipedia article … Continue reading

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Discovery of PF-04457845 (FAAH Inhibitor)


In this latest publication from the Pfizer labs, the authors describe their continuing efforts to identify urea-based, irreversible inhibitors of fatty acid amide hydrolase (FAAH).  Inhibition of FAAH and the concomitant elevation of endogenous levels of fatty acid amides has … Continue reading

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