New strong fibrates with piperidine moiety.
New fibrates containing piperidine, 4-hydroxypiperidine, piperidin-3-ene, and piperazine moieties in the structures were synthesized and evaluated. Among the synthesized compounds, 2-[3-[1-(4-fluorobenzoyl)-piperidin-4yl]phenoxyl-2-methylpropanoic acid (9aA: AHL-157) showed very superior activities in decreasing triglyceride, cholesterol, and blood sugar compared to bezafibrate in mice and rats.
Komoto
T
T
Central Research Labs, SSP Co, Ltd, Narita, Chiba, Japan. Teruo.Komoto@ssp.co.jp
Hirota
T K
TK
Otsuka
M
M
Kotake
J
J
Hasegawa
S
S
Koya
H
H
Sato
S
S
Sakamoto
T
T
D000818:Animals; D004195:Disease Models, Animal; D006937:Hypercholesterolemia / Q000188:drug therapy; D015228:Hypertriglyceridemia / Q000188:drug therapy; D007004:Hypoglycemic Agents / Q000138:chemical synthesis* / Q000737:chemistry / Q000627:therapeutic use; D000960:Hypolipidemic Agents / Q000138:chemical synthesis / Q000737:chemistry / Q000627:therapeutic use; D008297:Male; D051379:Mice; D008813:Mice, Inbred ICR; D000077489:Piperazine; D010879:Piperazines / Q000737:chemistry; D010880:Piperidines / Q000737:chemistry*; D011422:Propionates / Q000138:chemical synthesis* / Q000737:chemistry / Q000627:therapeutic use; D051381:Rats; D017207:Rats, Sprague-Dawley
D007004:Hypoglycemic Agents; D000960:Hypolipidemic Agents; D010879:Piperazines; D010880:Piperidines; D011422:Propionates; D000077489:Piperazine; C032727:piperidine