Structure-activity relationship for aryl and heteroaryl boronic acid inhibitors of hormone-sensitive lipase.
A range of aryl and heteroaryl boronic acids were tested for their in vitro hormone-sensitive lipase inhibitory properties. (2-Benzyloxy-5-fluorophenyl)boronic acid, (2-benzyloxy-5-chlorophenyl)boronic acid and 5-bromothiophene-2-boronic acid were found to be the most potent HSL inhibitors with IC(50) values of 140, 17 and 350 nM, respectively.
Ebdrup
Søren
S
Novo Nordisk A/S, Novo Nordisk Park, 2760 Måløv, Denmark. sebd@novonordisk.com
Jacobsen
Poul
P
Farrington
Anupma Dhanda
AD
Vedsø
Per
P
D000577:Amides / Q000737:chemistry; D001897:Boronic Acids / Q000138:chemical synthesis / Q000737:chemistry* / Q000494:pharmacology*; D004791:Enzyme Inhibitors / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology*; D020128:Inhibitory Concentration 50; D015394:Molecular Structure; D010636:Phenols / Q000737:chemistry; D002787:Sterol Esterase / Q000037:antagonists & inhibitors* / Q000378:metabolism; D013329:Structure-Activity Relationship; D013438:Sulfhydryl Compounds / Q000737:chemistry; D013455:Sulfur / Q000737:chemistry
D000577:Amides; D001897:Boronic Acids; D004791:Enzyme Inhibitors; D010636:Phenols; D013438:Sulfhydryl Compounds; D013455:Sulfur; D002787:Sterol Esterase