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Thiophene and bioisostere derivatives as new MMP12 inhibitors.
Badland, Matthew; Compère, Delphine; Courté, Karine; Dublanchet, Anne-Claude; Blais, Stéphane; Manage, Ajith; Peron, Guillaume; Wrigglesworth, Roger.
Bioorg Med Chem Lett ; 21(1): 528-30, 2011 Jan 01.
Article in English | MEDLINE | ID: mdl-21111619

ABSTRACT

A new MMP12 inhibitor series has been identified containing a thiophene moiety. Different approaches have been considered to replace this potential toxicophore. α-Fluorothiophene derivatives were the most interesting compounds. Their synthesis is presented.


Subject(s)
Matrix Metalloproteinase Inhibitors , Protease Inhibitors/chemistry , Thiophenes/chemistry , Matrix Metalloproteinase 12/metabolism , Protease Inhibitors/chemical synthesis , Protease Inhibitors/pharmacology , Structure-Activity Relationship , Thiophenes/chemical synthesis , Thiophenes/pharmacology
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