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Design and preparation of 2-benzamido-pyrimidines as inhibitors of IKK.
The design, synthesis, and the biological evaluation of 2-benzamido-pyrimidines as novel IKK inhibitors are described. By optimization of the lead compound 3, compounds 16 and 24 are identified asExpand
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Pyrrolo-pyrimidones: a novel class of MK2 inhibitors with potent cellular activity.
Pyrrolo-pyrimidones of the general structure 1 were synthesized and evaluated for their potential as MK2 inhibitors. Potent derivatives were discovered which inhibit MK2 in the nanomolar range andExpand
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Isolation and synthesis of a novel immunosuppressive 17alpha-substituted dammarane from the flour of the Palmyrah palm (Borassus flabellifer).
The novel triterpene 1 with a dammarane skeleton and a hitherto unknown 17alpha-substitution pattern has been isolated from the Palmyrah palm in low yield and prepared by synthesis in largerExpand
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Novel p38 inhibitors with potent oral efficacy in several models of rheumatoid arthritis.
A library of trisubstituted oxazoles, thiazoles, imidazoles (1,2,4- and 2,4,5-substituted) and imidazo[1,2-b]pyridines was prepared and evaluated in vitro as p38alpha inhibitors and in vivo inExpand
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Novel 3-aminopyrazole inhibitors of MK-2 discovered by scaffold hopping strategy.
New, selective 3-aminopyrazole based MK2-inhibitors were discovered by scaffold hopping strategy. The new derivatives proved to inhibit intracellular phosphorylation of hsp27 as well as LPS-inducedExpand
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Design and synthesis of novel ligands for the 5-HT3 and the 5-HT4 receptor
Abstract A novel highly potent 5-HT3 antagonist and Tropisetron analogue ( 1 is described with an increased efficacy to inhibit cisplatin induced emesis in ferrets. Four novel structural classes ofExpand
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Synthesis of P1 aspartate-based peptide acyloxymethyl and fluoromethyl ketones as inhibitors of interleukin-1β-converting enzyme
Abstract Improved procedures have been developed for the synthesis of P1 aspartate-based 2,6-dichlorobenzoyloxymethyl ketone 1 and fluoromethyl ketone 2 , the prodrugs of two potent ICE-inhibitors. 1Expand
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Reduction of inflammation and pyrexia in the rat by oral administration of SDZ 224‐015, an inhibitor of the interleukin‐1β converting enzyme
1 The aim of this study was to determine whether a synthetic inhibitor of the interleukin‐1β converting enzyme (ICE) displays oral activity in models of inflammation. 2 To this end, the ICEExpand
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N-aryl-piperidine-4-carboxamides as a novel class of potent inhibitors of MALT1 proteolytic activity.
Starting from a weak screening hit, potent and selective inhibitors of the MALT1 protease function were elaborated. Advanced compounds displayed high potency in biochemical and cellular assays.Expand
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