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Bioorg Med Chem Lett. 1998 Aug 18;8(16):2203-8.

Isoxazolylthioamides as potential immunosuppressants a combinatorial chemistry approach.

Author information

1
Novartis Pharma AG, Basel, Switzerland. rainer.albert@pharma.novartis.com

Abstract

A library of thioamide derivatives of leflunomide 1a and of its bioactive metabolite 1b has been synthesised on solid phase. Thus, para-substituted phenylacetic acids were coupled to TentaGel and were subsequently reacted with aromatic isothiocyanates. Treatment of the resulting enaminothioamides with hydroxylamine led to their simultaneous cyclisation and cleavage from the resin affording 2-25. Their in vitro profiling demonstrated that the amide-thioamide isologous substitution was detrimental of the biological activity.

PMID:
9873513
DOI:
10.1016/s0960-894x(98)00365-5
[Indexed for MEDLINE]

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