| Autor: |
Shirley M. Williams, Robert G. Aslanian, Christopher Sondey, Sylvia J. Degrado, Ning Shao, Mary Senior, Li Wang, Shuqin Zheng, Joyce J. Hwa, Robert E. West, Ren-Long Wu, Ashwin U. Rao, Anandan Palani, Bhuneshwari Patel, Mckittrick Brian A, Tin-Yau Chan |
| Rok vydání: |
2011 |
| Předmět: |
|
| Zdroj: |
ACS Medicinal Chemistry Letters. 3:198-202 |
| ISSN: |
1948-5875 |
| DOI: |
10.1021/ml200250t |
| Popis: |
A series of novel 2-piperidinopiperidine thiadiazoles were synthesized and evaluated as new leads of histamine H3 receptor antagonists. The 4-(5-([1,4'-bipiperidin]-1'-yl)-1,3,4-thiadiazol-2-yl)-2-(pyridin-2-yl)morpholine (5u) displayed excellent potency and ex vivo receptor occupancy. Compound 5u was also evaluated in vivo for antidiabetic efficacy in STZ diet-induced obesity type 2 diabetic mice for 2 or 12 days. Non-fasting glucose levels were significantly reduced as compared with vehicle-treated mice. In addition, 5u dose dependently blocked the increase of HbA1c after 12 days of treatment. |
| Databáze: |
OpenAIRE |
| Externí odkaz: |
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