Abstract

Inhibitors of dipeptidyl peptidase-4 (DPP4) have been shown to be effective treatments for type 2 diabetes. A series of novel 1,2,3-triazole based xanthine derivatives were designed and evaluated for in vitro dipeptidyl peptidase-4 (DPP-4) activity. Among them, the representative compounds 7b, 7e, 7g and 6e showed excellent inhibitory activity of DPP-4 with IC₅₀ values ranging from 87.41 to 16.34 nM, respectively. The SAR of these xanthine derivatives have been discussed, which would be useful for developing novel DPP-4 inhibitors as treating type 2 diabetes.

Graphic Abstract

1,2,3-triazole based xanthine derivatives were designed and evaluated for in vitro dipeptidyl peptidase-4 (DPP-4) activity. The SAR of these xanthine derivatives had been discussed, which would be useful for developing novel DPP-4 inhibitors as treating type 2 diabetes.

中文翻译：

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新型1,2,3-三唑基黄嘌呤衍生物作为DPP-4抑制剂的设计，合成和生物学评价

摘要

二肽基肽酶-4（DPP4）抑制剂已被证明是2型糖尿病的有效治疗方法。设计了一系列新颖的基于1,2,3-三唑的黄嘌呤衍生物，并对其体外二肽基肽酶-4（DPP-4）活性进行了评估。其中，代表性化合物7b，7e，7g和6e表现出优异的DPP-4抑制活性，IC ₅₀值分别为87.41至16.34 nM。已经讨论了这些黄嘌呤衍生物的SAR，这将有助于开发新型DPP-4抑制剂来治疗2型糖尿病。

图形摘要

设计基于1,2,3-三唑的黄嘌呤衍生物，并评估其体外二肽基肽酶-4（DPP-4）活性。已经讨论了这些黄嘌呤衍生物的SAR，这将有助于开发新型DPP-4抑制剂来治疗2型糖尿病。