Design and synthesis of novel bis-oximinoalkanoic acids as potent PPAR alpha agonists.
Bis-oximinoalkanoic acid derivatives were designed and synthesized to aid in the characterization of selective PPARalpha agonists by replacing the oxazole ring with flexible oximino group in the lipophilic tail part of a previously reported compound 3. Selected compounds 9d and 9m showed excellent potency and high selectivity towards PPARalpha in vitro. These compounds found effective in reducing serum triglycerides (TG) in vivo.
Pingali
Harikishore
H
Zydus Research Centre, Sarkhej-Bavla NH 8A Moraiya, Ahmedabad 382 210, India. pingalihk@rediffmail.com
Jain
Mukul
M
Shah
Shailesh
S
Zaware
Pandurang
P
Makadia
Pankaj
P
Pola
Suresh
S
Thube
Baban
B
Patel
Darshit
D
Patil
Pravin
P
Priyadarshini
Priyanka
P
Suthar
Dinesh
D
Shah
Maanan
M
Giri
Suresh
S
Patel
Pankaj
P
D000098:Acetophenones / Q000138:chemical synthesis; D000473:Alkanes / Q000138:chemical synthesis*; D000818:Animals; D015195:Drug Design; D006801:Humans; D000960:Hypolipidemic Agents / Q000138:chemical synthesis* / Q000378:metabolism; D051379:Mice; D010080:Oxazoles / Q000138:chemical synthesis*; D047493:PPAR alpha / Q000819:agonists* / Q000378:metabolism; D014280:Triglycerides / Q000378:metabolism
D000098:Acetophenones; D000473:Alkanes; D000960:Hypolipidemic Agents; D010080:Oxazoles; D047493:PPAR alpha; D014280:Triglycerides; C038699:acetophenone