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Discovery of a potent thiadiazole class of histamine h3 receptor antagonist for the treatment of diabetes.
Rao, Ashwin U; Shao, Ning; Aslanian, Robert G; Chan, Tin-Yau; Degrado, Sylvia J; Wang, Li; McKittrick, Brian; Senior, Mary; West, Robert E; Williams, Shirley M; Wu, Ren-Long; Hwa, Joyce; Patel, Bhuneshwari; Zheng, Shuqin; Sondey, Christopher; Palani, Anandan.
Afiliación
  • Rao AU; Department of Medicinal Chemistry and Cardiovascular/Metabolic Disease, Merck Research Laboratories , 2015 Galloping Hill Road, Kenilworth, New Jersey 07033, United States.
  • Shao N; Department of Medicinal Chemistry and Cardiovascular/Metabolic Disease, Merck Research Laboratories , 2015 Galloping Hill Road, Kenilworth, New Jersey 07033, United States.
  • Aslanian RG; Department of Medicinal Chemistry and Cardiovascular/Metabolic Disease, Merck Research Laboratories , 2015 Galloping Hill Road, Kenilworth, New Jersey 07033, United States.
  • Chan TY; Department of Medicinal Chemistry and Cardiovascular/Metabolic Disease, Merck Research Laboratories , 2015 Galloping Hill Road, Kenilworth, New Jersey 07033, United States.
  • Degrado SJ; Department of Medicinal Chemistry and Cardiovascular/Metabolic Disease, Merck Research Laboratories , 2015 Galloping Hill Road, Kenilworth, New Jersey 07033, United States.
  • Wang L; Department of Medicinal Chemistry and Cardiovascular/Metabolic Disease, Merck Research Laboratories , 2015 Galloping Hill Road, Kenilworth, New Jersey 07033, United States.
  • McKittrick B; Department of Medicinal Chemistry and Cardiovascular/Metabolic Disease, Merck Research Laboratories , 2015 Galloping Hill Road, Kenilworth, New Jersey 07033, United States.
  • Senior M; Department of Medicinal Chemistry and Cardiovascular/Metabolic Disease, Merck Research Laboratories , 2015 Galloping Hill Road, Kenilworth, New Jersey 07033, United States.
  • West RE; Department of Medicinal Chemistry and Cardiovascular/Metabolic Disease, Merck Research Laboratories , 2015 Galloping Hill Road, Kenilworth, New Jersey 07033, United States.
  • Williams SM; Department of Medicinal Chemistry and Cardiovascular/Metabolic Disease, Merck Research Laboratories , 2015 Galloping Hill Road, Kenilworth, New Jersey 07033, United States.
  • Wu RL; Department of Medicinal Chemistry and Cardiovascular/Metabolic Disease, Merck Research Laboratories , 2015 Galloping Hill Road, Kenilworth, New Jersey 07033, United States.
  • Hwa J; Department of Medicinal Chemistry and Cardiovascular/Metabolic Disease, Merck Research Laboratories , 2015 Galloping Hill Road, Kenilworth, New Jersey 07033, United States.
  • Patel B; Department of Medicinal Chemistry and Cardiovascular/Metabolic Disease, Merck Research Laboratories , 2015 Galloping Hill Road, Kenilworth, New Jersey 07033, United States.
  • Zheng S; Department of Medicinal Chemistry and Cardiovascular/Metabolic Disease, Merck Research Laboratories , 2015 Galloping Hill Road, Kenilworth, New Jersey 07033, United States.
  • Sondey C; Department of Medicinal Chemistry and Cardiovascular/Metabolic Disease, Merck Research Laboratories , 2015 Galloping Hill Road, Kenilworth, New Jersey 07033, United States.
  • Palani A; Department of Medicinal Chemistry and Cardiovascular/Metabolic Disease, Merck Research Laboratories , 2015 Galloping Hill Road, Kenilworth, New Jersey 07033, United States.
ACS Med Chem Lett ; 3(3): 198-202, 2012 Mar 08.
Article en En | MEDLINE | ID: mdl-24900450
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.
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Texto completo: 1 Colección: 01-internacional Base de datos: MEDLINE Idioma: En Revista: ACS Med Chem Lett Año: 2012 Tipo del documento: Article País de afiliación: Estados Unidos Pais de publicación: Estados Unidos
Texto completo
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Texto completo: 1 Colección: 01-internacional Base de datos: MEDLINE Idioma: En Revista: ACS Med Chem Lett Año: 2012 Tipo del documento: Article País de afiliación: Estados Unidos Pais de publicación: Estados Unidos