Back to Search
Start Over
Discovery of a potent thiadiazole class of histamine h3 receptor antagonist for the treatment of diabetes.
- Source :
-
ACS medicinal chemistry letters [ACS Med Chem Lett] 2011 Nov 21; Vol. 3 (3), pp. 198-202. Date of Electronic Publication: 2011 Nov 21 (Print Publication: 2012). - Publication Year :
- 2011
-
Abstract
- 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.
Details
- Language :
- English
- ISSN :
- 1948-5875
- Volume :
- 3
- Issue :
- 3
- Database :
- MEDLINE
- Journal :
- ACS medicinal chemistry letters
- Publication Type :
- Academic Journal
- Accession number :
- 24900450
- Full Text :
- https://doi.org/10.1021/ml200250t