Thiophene and bioisostere derivatives as new MMP12 inhibitors.
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.
Evotec OAI, 151 Milton Park, Abingdon, Oxon OX14 SD, UK. matthew.badland@pfizer.com
Matthew
M
Badland
Delphine
D
Compère
Karine
K
Courté
Anne-Claude
AC
Dublanchet
Stéphane
S
Blais
Ajith
A
Manage
Guillaume
G
Peron
Roger
R
Wrigglesworth
D053508:Matrix Metalloproteinase 12 / Q000378:metabolism; D061965:Matrix Metalloproteinase Inhibitors; D011480:Protease Inhibitors / Q000138:chemical synthesis / Q000737:chemistry* / Q000494:pharmacology; D013329:Structure-Activity Relationship; D013876:Thiophenes / Q000138:chemical synthesis / Q000737:chemistry* / Q000494:pharmacology
D061965:Matrix Metalloproteinase Inhibitors; D011480:Protease Inhibitors; D013876:Thiophenes; D053508:Matrix Metalloproteinase 12