Potent inhibitors of the Qi site of the mitochondrial respiration complex III.
A series of azole-fused salicylamides were prepared as analogues of antimycin and assayed for activity at complex III of the mitochondrial respiratory chain. The activity of these compounds approached that of antimycin in inhibitory potency and some showed growth reduction of Septoria nodorum in vitro. Compound 8a was shown to bind at the Qi site of complex III by red-shift titration of the bc1 complex.
Bolgunas
Stephen
S
DuPont Agricultural Products, Stine/Haskell Research Center, Post Office Box 30, Newark, Delaware 19714, USA.
Clark
David A
DA
Hanna
Wayne S
WS
Mauvais
Patricia A
PA
Pember
Steve O
SO
D000968:Antimycin A / Q000031:analogs & derivatives* / Q000138:chemical synthesis* / Q000494:pharmacology; D001203:Ascomycota / Q000187:drug effects; D001393:Azoles / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology; D014450:Electron Transport Complex III / Q000037:antagonists & inhibitors*; D005659:Fungicides, Industrial / Q000138:chemical synthesis / Q000494:pharmacology; D012457:Salicylamides / Q000138:chemical synthesis* / Q000494:pharmacology; D013329:Structure-Activity Relationship
D001393:Azoles; D005659:Fungicides, Industrial; D012457:Salicylamides; D000968:Antimycin A; D014450:Electron Transport Complex III