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2004
Pyrrole derivatives
R 0120
Synthesis and Structure—Activity Relationship of a Novel Sulfone Series of
Converting Enzyme Inhibitors. — The amide functionality in IM491, one of
52- 094 TNF-α
the most effective TNF-α converting enzyme inhibitors reported so far, is replaced by
a sulfonyl group yielding a new series of α,β-cyclic and β,β-cyclic γ-sulfonyl hydroxamic acids. All compounds prepared contain a basic piperidine or pyrrolidine nitrogen
to maintain the good water solubility and low protein binding of the parent compound.
The best analogue (XIV) is asymmetrically synthesized from aspartic acid (I). Most of
the sulfones are more potent than IM491 in porcine TACE assay with similar selectivity
profile over MMPs, but less potent in the inhibition of TNF-α production in WBA.
— (XUE*, C.-B.; CHEN*, X.-T.; et al.; Bioorg. Med. Chem. Lett. 14 (2004) 17,
4453-4459; Bristol-Myers Squibb Pharm. Res. Inst., Princeton, NJ 08543, USA;
Eng.) — H. Hoennerscheid
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