Simplified YM-26734 inhibitors of secreted phospholipase A2 group IIA.
Simplified analogs of YM-26734, a known inhibitor of secreted phospholipase A(2) (sPLA(2)) group IIA, were synthesized and found to also display potent inhibition at low nanomolar concentrations. Analogs were based on the didodecanoylphloroglucinol portion of YM-26734 which contains the predicted active site calcium binding group.
Oslund
Rob C
RC
Department of Chemistry, Campus Box 351700, University of Washington, Seattle, WA 98195, USA.
Cermak
Nathan
N
Verlinde
Christophe L M J
CL
Gelb
Michael H
MH
D000818:Animals; D002118:Calcium / Q000737:chemistry; D020134:Catalytic Domain; D002626:Chemistry, Pharmaceutical / Q000379:methods*; D002839:Chromans / Q000037:antagonists & inhibitors* / Q000494:pharmacology*; D015195:Drug Design; D054501:Group II Phospholipases A2 / Q000037:antagonists & inhibitors*; D006801:Humans; D007211:Indoles / Q000737:chemistry; D020128:Inhibitory Concentration 50; D051379:Mice; D008962:Models, Theoretical; D010636:Phenols / Q000037:antagonists & inhibitors* / Q000494:pharmacology*; D011485:Protein Binding; D051381:Rats
D002839:Chromans; D007211:Indoles; D010636:Phenols; C084181:YM 26734; C030374:indole; D054501:Group II Phospholipases A2; D002118:Calcium