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首页> 外文期刊>European Journal of Medicinal Chemistry: Chimie Therapeutique >Synthesis, biological assay in vitro and molecular docking studies of new imidazopyrazinone derivatives as potential dipeptidyl peptidase IV inhibitors.
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Synthesis, biological assay in vitro and molecular docking studies of new imidazopyrazinone derivatives as potential dipeptidyl peptidase IV inhibitors.

机译：新型咪唑嗪衍生物作为潜在二肽肽肽酶IV抑制剂的合成，生物学测定和新的咪唑嗪衍生物的分子对接研究。

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摘要

A series of novel imidazopyrazinone derivatives were synthesized and evaluated with regard to their ability to inhibit dipeptidyl peptidase IV (DPP-IV) in vitro. Of these compounds (2R)-4-oxo-4-[2-(3-carbamoylbenzyl)-hexahydro-3-oxoimidazo [1,5-a]pyrazin-7(8H)-yl]-1-(2,4,5-trifluorophenyl)butan-2-amine fumaric acid (17h, IC(50)=78 nM) was shown to effectively inhibit the activity of the dipeptidyl peptidase IV enzyme. Molecular docking studies were also performed to illustrate the binding mode of compounds 15c and 17h. Favorable interactions were identified from the binding of inhibitor 15c with DPP-IV. By analogy to the binding mode of compound 15c, it seems that the introduction of a substituted benzyl moiety onto the imidazopyrazinone could remarkably improve the inhibitory activity of compound 17h.
机译：合成了一系列新的咪唑嗪酮衍生物，并在体外抑制二肽基肽酶IV（DPP-IV）的能力。 这些化合物（2R）-4-氧代-4- [2-（3-氨基甲酰基苄基）-HEXAHYDRO-3-氧代咪唑[1,5-a]吡嗪-7（8h） - ~1-（2,4 ，5-三氟苯基）丁烷-2-胺富马酸（17H，IC（50）= 78nm）有效抑制二肽基肽酶IV酶的活性。 还进行了分子对接研究以说明化合物15C和17H的结合模式。 从抑制剂15C与DPP-IV的结合鉴定有利的相互作用。 通过类似于化合物15c的结合方式，似乎将取代的苄基部分引入咪唑嗪酮上可以显着改善化合物17h的抑制活性。

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