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Anglický jazyk
Novel 4-Heteroaryl-Antipyrines as DPP-IV Inhibitors
Autor: Mohamed Abdalla
Type 2 diabetes mellitus is a progressive disease that affects almost 8.3% of global population. Regardless the availability of vast variety of oral hypoglycemics, only 36% of patients achieves proper glycemic control. With the advantage of low risk of hypoglycemia,... Viac o knihe
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O knihe
Type 2 diabetes mellitus is a progressive disease that affects almost 8.3% of global population. Regardless the availability of vast variety of oral hypoglycemics, only 36% of patients achieves proper glycemic control. With the advantage of low risk of hypoglycemia, DPP-IV attracted the attention of medicinal chemists as a new target for oral hypoglycemics. In this report, a lead compound 1, with antipyrine scaffold, was obtained, and its binding mode was calculated. Several derivatives with bridged nitrogenous heterocycles have been synthesized via multi-component reaction under controlled microwave heating conditions. The antidiabetic activity vs. DPP-IV protein was evaluated and compared with sitagliptin. Compounds with small or medium sized nitrogenous bridges were comparable with sitagliptin in term of DPP-IV inhibitory activity, potentially via targeting Glu203 and Glu204. The oral hypoglycemic activities of compounds with submicromolar IC50 values were further evaluated using diabetic mouse model.
- Vydavateľstvo: LAP LAMBERT Academic Publishing
- Rok vydania: 2017
- Formát: Paperback
- Rozmer: 220 x 150 mm
- Jazyk: Anglický jazyk
- ISBN: 9783659800290
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