Solid-phase synthesis of an arylsulfone hydroxamate library.
Synthesis of an arylsulfone hydroxamate lead optimization library is presented. Biological activity of representative examples is given to demonstrate the value of this approach for lead optimization.
Rhone Poulenc Rorer, Lead Discovery Department, Collegeville, PA 19426, USA. Jsalvino@aol.com
J M
JM
Salvino
R
R
Mathew
T
T
Kiesow
R
R
Narensingh
H J
HJ
Mason
A
A
Dodd
R
R
Groneberg
C J
CJ
Burns
G
G
McGeehan
J
J
Kline
E
E
Orton
S Y
SY
Tang
M
M
Morrisette
R
R
Labaudininiere
D015105:3',5'-Cyclic-AMP Phosphodiesterases / Q000037:antagonists & inhibitors; D054703:Cyclic Nucleotide Phosphodiesterases, Type 4; D004791:Enzyme Inhibitors / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology; D006877:Hydroxamic Acids / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology; D061965:Matrix Metalloproteinase Inhibitors; D013329:Structure-Activity Relationship; D013450:Sulfones / Q000737:chemistry*
D004791:Enzyme Inhibitors; D006877:Hydroxamic Acids; D061965:Matrix Metalloproteinase Inhibitors; D013450:Sulfones; D015105:3',5'-Cyclic-AMP Phosphodiesterases; D054703:Cyclic Nucleotide Phosphodiesterases, Type 4