Autor: |
Becker DP; Departments of Medicinal Chemistry and Inflammation-Oncology, Pharmacia Research & Development, 4901 Searle Parkway, Skokie, IL 60077, USA. daniel.p.becker@pharmacia.com, Barta TE, Bedell L, DeCrescenzo G, Freskos J, Getman DP, Hockerman SL, Li M, Mehta P, Mischke B, Munie GE, Swearingen C, Villamil CI |
Jazyk: |
angličtina |
Zdroj: |
Bioorganic & medicinal chemistry letters [Bioorg Med Chem Lett] 2001 Oct 22; Vol. 11 (20), pp. 2719-22. |
DOI: |
10.1016/s0960-894x(01)00556-x |
Abstrakt: |
A series of alpha-amino-beta-sulphone hydroxamates was prepared and evaluated for potency versus MMP-13 and selectivity versus MMP-1. Various substituents were employed on the alpha-amino group (P(1) position), as well as different groups attached to the sulphone group extending into P(1)'. Low nanomolar potency was obtained for MMP-13 with selectivity versus MMP-1 of >1000x for a number of analogues. |
Databáze: |
MEDLINE |
Externí odkaz: |
|