Synthesis and pharmacological profile of serofendic acids A and B.
We present efficient syntheses of serofendic acids A and B (SA-A and SA-B), novel neuroprotective substances isolated from fetal calf serum. Biological and pharmacological evaluation showed that SA-A and SA-B have potent protective action against glutamate-induced neurotoxicity, but do not interact directly with glutamate receptors. A pharmacokinetic study showed that they have good oral bioavailability in rats. The results indicate that SA-A and SA-B are potential lead compounds for candidate drugs to treat various neurological disorders.
Terauchi
Taro
T
Tsukuba Research Laboratories, Eisai Co., Ltd, Tsukuba-shi 300-2635, Japan. t-terauchi@hhc.eisai.co.jp
Asai
Naoki
N
Doko
Takashi
T
Taguchi
Ryota
R
Takenaka
Osamu
O
Sakurai
Hideki
H
Yonaga
Masahiro
M
Kimura
Teiji
T
Kajiwara
Akiharu
A
Niidome
Tetsuhiro
T
Kume
Toshiaki
T
Akaike
Akinori
A
Sugimoto
Hachiro
H
D000284:Administration, Oral; D000818:Animals; D002417:Cattle; D002470:Cell Survival / Q000187:drug effects; D002478:Cells, Cultured; D002540:Cerebral Cortex / Q000166:cytology; D018360:Crystallography, X-Ray; D004224:Diterpenes / Q000008:administration & dosage / Q000138:chemical synthesis* / Q000494:pharmacology*; D004305:Dose-Response Relationship, Drug; D004353:Drug Evaluation, Preclinical; D005312:Fetal Blood / Q000737:chemistry; D018698:Glutamic Acid / Q000633:toxicity; D007275:Injections, Intravenous; D008958:Models, Molecular; D008968:Molecular Conformation; D009474:Neurons / Q000166:cytology / Q000187:drug effects; D018696:Neuroprotective Agents / Q000008:administration & dosage / Q000138:chemical synthesis* / Q000494:pharmacology*; D051381:Rats; D017207:Rats, Sprague-Dawley; D013237:Stereoisomerism; D013329:Structure-Activity Relationship; D014018:Tissue Distribution