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
Main Authors: Zask, A., Gu, Y., Albright, J.D., Du, X., Hogan, M., Levin, J.I., Chen, J.M., Killar, L.M., Sung, A., DiJoseph, J.F., Sharr, M.A., Roth, C.E., Skala, S., Jin, G., Cowling, R., Mohler, K.M., Barone, D., Black, R., March, C., Skotnicki, J.S.
Format: Journal Article
Language:English
Published: Oxford Elsevier Ltd 17-04-2003
Elsevier
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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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ISSN:0960-894X
1464-3405
DOI:10.1016/S0960-894X(03)00127-6