Hit to lead SAR study on benzoxazole derivatives for an NPY Y5 antagonist.
We report a hit to lead study on a novel benzoxazole NPY Y5 antagonist. Starting from HTS hit 1, structure-activity relationships were developed. Compound 12 showed reduction of food intake and a tendency to suppress body weight gain over the 21-day experimental period.
Medicinal Research Laboratories, Shionogi & Co., Ltd, 1-1, Futaba-cho 3-chome, Toyonaka, Osaka 561-0825, Japan. naoki.oomori@shionogi.co.jp
Naoki
N
Omori
Naoki
N
Kouyama
Akira
A
Yukimasa
Kana
K
Watanabe
Yasunori
Y
Yokota
Hideki
H
Tanioka
Hirohide
H
Nambu
Hideo
H
Yukioka
Norihito
N
Sato
Yukari
Y
Tanaka
Kazutaka
K
Sekiguchi
Takayuki
T
Okuno
D000818:Animals; D019440:Anti-Obesity Agents / Q000737:chemistry* / Q000493:pharmacokinetics / Q000494:pharmacology / Q000627:therapeutic use*; D001583:Benzoxazoles / Q000737:chemistry* / Q000493:pharmacokinetics / Q000494:pharmacology / Q000627:therapeutic use*; D001835:Body Weight / Q000187:drug effects; D004435:Eating / Q000187:drug effects; D006801:Humans; D051379:Mice; D009765:Obesity / Q000188:drug therapy* / Q000378:metabolism; D051381:Rats; D017476:Receptors, Neuropeptide Y / Q000037:antagonists & inhibitors* / Q000378:metabolism; D013329:Structure-Activity Relationship
D019440:Anti-Obesity Agents; D001583:Benzoxazoles; D017476:Receptors, Neuropeptide Y; C100568:neuropeptide Y5 receptor