Design and Synthesis of Potential Macrocyclic Zinc Metalloprotease Inhibitors
โ Scribed by Bao-Xiang Zhao; Marco Schaudt; Siegfried Blechert
- Publisher
- John Wiley and Sons
- Year
- 2006
- Tongue
- English
- Weight
- 82 KB
- Volume
- 24
- Category
- Article
- ISSN
- 0256-7660
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โฆ Synopsis
A series of succinate-derived macrocyclic amides 1 were synthezized using ring-closing metathesis in the key step. The substrate scope includes rings of 11 to 14 members. The cyclic dicarboxylic acids 1 represent a family of new model compounds for potential zinc metalloprotease inhibitors. The metathesis precursors were provided by amide coupling of tert-butyl 3-carboxyhex-5-enoate 2 with numerous side chain alkenylated amino acid esters of general type 3 derived from L-tyrosine and L-cysteine.
๐ SIMILAR VOLUMES
Dethiobiotin synthetase (DTBS ; E.C. 6.6.6.6), the penultimate enzyme in the biosynthesis of the essential vitamin biotin, is a new potential target for novel herbicides. Inhibitors were designed based on mechanistic and structural information. The in-vitro activities of these potential inhibitors v