{"product_id":"novel-4-heteroaryl-antipyrines-as-dpp-iv-inhibitors-von-mohamed-abdalla","title":"Novel 4-Heteroaryl-Antipyrines as DPP-IV Inhibitors","description":"\u003cp\u003eType 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.\u003c\/p\u003e\u003cdiv class=\"aw-variant-hidden-subtitle-div\" id=\"aw-variant-subtitle-9783659800290\"\u003e\u003ch3\u003e\u003c\/h3\u003e\u003c\/div\u003e","brand":"Libri","offers":[{"title":"Softcover - 9783659800290","offer_id":39450538770525,"sku":"9783659800290","price":35.9,"currency_code":"EUR","in_stock":true}],"thumbnail_url":"\/\/cdn.shopify.com\/s\/files\/1\/0940\/0622\/files\/6103e16c-1e61-4429-a2a9-b8fe5d3ef137.jpg?v=1773726955","url":"https:\/\/shop.autorenwelt.de\/products\/novel-4-heteroaryl-antipyrines-as-dpp-iv-inhibitors-von-mohamed-abdalla","provider":"Autorenwelt Shop","version":"1.0","type":"link"}