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Deprecated: Implicit conversion from float 231.6 to int loses precision in C:\Inetpub\vhosts\kidney.de\httpdocs\pget.php on line 534 ACS+Med+Chem+Lett 2012 ; 3 (3): 198-202 Nephropedia Template TP
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Discovery of a Potent Thiadiazole Class of Histamine H3 Receptor Antagonist for the Treatment of Diabetes #MMPMID24900450
Rao AU; Shao N; Aslanian R; Chan TY; Degrado SJ; Wang L; McKittrick B; Senior M; West RE; Williams SM; Wu RL; Hwa J; Patel B; Zheng S; Sondey C; Palani A
ACS Med Chem Lett 2012[Mar]; 3 (3): 198-202 PMID24900450show ga
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.