Development of rhodesain inhibitors with a 3-bromoisoxazoline warhead.
نویسندگان
چکیده
Novel rhodesain inhibitors were obtained by combining an enantiomerically pure 3-bromoisoxazoline warhead with a specific peptidomimetic recognition moiety. All derivatives behaved as inhibitors of rhodesain, with low micromolar Ki values. Their activity against the enzyme was found to be paralleled by an in vitro antitrypanosomal activity, with IC50 values in the mid-micromolar range. Notably, a preference for parasitic over human proteases, specifically cathepsins B and L, was observed.
منابع مشابه
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ورودعنوان ژورنال:
- ChemMedChem
دوره 8 12 شماره
صفحات -
تاریخ انتشار 2013