Synthesis and SAR of bicyclic heteroaryl hydroxamic acid MMP and TACE inhibitors
Potent and selective bicyclic heteroaryl hydroxamic acid MMP and TACE inhibitors were synthesized by a novel convergent route. Selectivity and efficacy versus MMPs and TACE could be controlled by appropriate substitution on the scaffolds and by variation of the P1′ group. Select compounds were found...
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Published in: | Bioorganic & medicinal chemistry letters Vol. 13; no. 8; pp. 1487 - 1490 |
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Main Authors: | , , , , , , , , , , , , , , , , , , , |
Format: | Journal Article |
Language: | English |
Published: |
Oxford
Elsevier Ltd
17-04-2003
Elsevier |
Subjects: | |
Online Access: | Get full text |
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Summary: | Potent and selective bicyclic heteroaryl hydroxamic acid MMP and TACE inhibitors were synthesized by a novel convergent route. Selectivity and efficacy versus MMPs and TACE could be controlled by appropriate substitution on the scaffolds and by variation of the P1′ group. Select compounds were found to be effective in in vivo models of arthritis.
Potent and selective bicyclic heteroaryl hydroxamic acid MMP and TACE inhibitors were synthesized by a novel convergent route. Selectivity and efficacy versus MMPs and TACE could be controlled by appropriate substitution on the scaffolds and by variation of the P1′ group. Select compounds were found to be effective in in vivo models of arthritis. |
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Bibliography: | ObjectType-Article-1 SourceType-Scholarly Journals-1 ObjectType-Feature-2 content type line 23 |
ISSN: | 0960-894X 1464-3405 |
DOI: | 10.1016/S0960-894X(03)00127-6 |