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Volumn 20, Issue 15, 2010, Pages 4395-4398

Synthesis and SAR of azolopyrimidines as potent and selective dipeptidyl peptidase-4 (DPP4) inhibitors for type 2 diabetes

Author keywords

Azolopyrimidines; DPP4; GLP 1; SAR

Indexed keywords

ALOGLIPTIN; AZOLOPYRIMIDINE; DIPEPTIDYL PEPTIDASE IV INHIBITOR; LINAGLIPTIN; SAXAGLIPTIN; SITAGLIPTIN; UNCLASSIFIED DRUG; VILDAGLIPTIN;

EID: 77955367308     PISSN: 0960894X     EISSN: None     Source Type: Journal    
DOI: 10.1016/j.bmcl.2010.06.063     Document Type: Article
Times cited : (56)

References (23)
  • 1
    • 84855628671 scopus 로고    scopus 로고
    • Diabetes Facts and Figures October 6
    • Diabetes Facts and Figures. International Diabetes Foundation, October 6, 2009. http://www.idf.org/Facts-and-Figures.
    • (2009) International Diabetes Foundation
  • 3
    • 84855639125 scopus 로고    scopus 로고
    • For latest information, please visit the website of World Health Organization at
    • For latest information, please visit the website of World Health Organization at http://www.who.int/diabetes/facts/world-figures/en/.
  • 19
    • 61349143225 scopus 로고    scopus 로고
    • For other small molecular DPP-IV inhibitors, see: S.H. Havale, and M. Pal Bioorg. Med. Chem. 17 2009 1783 and references cited therein
    • (2009) Bioorg. Med. Chem. , vol.17 , pp. 1783
    • Havale, S.H.1    Pal, M.2
  • 23
    • 77955419687 scopus 로고    scopus 로고
    • note
    • Oral glucose tolerance test in ob/ob mice. Male 13-14 weeks old ob/ob mice (Jackson Labs) were maintained under constant temperature and humidity conditions, a 12 h:12 h light-dark cycle, and had free access to a 10% fat rodent diet (D1245B Research Diets) and tap water. After an overnight fasting period, animals were dosed orally with vehicle (water) or DPP4 inhibitor (3 and 10 μmol/kg) at -60 min. Two blood samples were collected at -60 and 0 min by tail bleed for glucose and insulin determinations. Glucose (2 g/kg) was then administered orally (at 0 min). Additional blood samples were collected at 15, 30, 60, 90, and 120 min for glucose and insulin determinations. Blood samples were collected into EDTA containing tubes (Sarstedt). Plasma insulin was assayed using a mouse insulin ELISA kit (ALPCO Diagnostics). Data represent the mean of 12-24 mice/group. All procedures were performed according to BMS-IACUC guidelines.


* 이 정보는 Elsevier사의 SCOPUS DB에서 KISTI가 분석하여 추출한 것입니다.