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某些尿嘧啶衍生物的碳酸酐酶抑制特性

Carbonic anhydrase inhibitory properties of some uracil derivatives.

作者信息

Alper Türkoğlu Emir, Şentürk Murat, Supuran Claudiu T, Ekinci Deniz

机构信息

a Department of Pharmaceutical Technology , Agri Ibrahim Cecen University , Agri , Turkey.

b Department of Chemistry , Agri Ibrahim Cecen University , Agri , Turkey.

出版信息

J Enzyme Inhib Med Chem. 2017 Dec;32(1):74-77. doi: 10.1080/14756366.2016.1235043.

Abstract

Inhibitors of carbonic anhydrase (CA) have been carried out in many therapeutic applications, especially antiglaucoma activity. In this study, we investigated some uracil derivatives (4-12) to inhibit human CA I (hCA I) and II (hCA II) isoenzymes. The K values of the compounds 4-12 are in the range of 0.085-428 µM for hCA I and of 0.1715-645 µM against hCA II, respectively. It is concluded from the kinetic investigations, all compounds used in the study act as competitive inhibitors with substrate, 4-NPA. Uracil derivatives are emerging agents for the inhibiton of carbonic anhydrase which could be used in biomedicine.

摘要

碳酸酐酶(CA)抑制剂已被应用于许多治疗领域,尤其是抗青光眼活性方面。在本研究中,我们研究了一些尿嘧啶衍生物(4 - 12)对人碳酸酐酶I(hCA I)和II(hCA II)同工酶的抑制作用。化合物4 - 12对hCA I的K值范围为0.085 - 428 μM,对hCA II的K值范围为0.1715 - 645 μM。动力学研究得出结论,该研究中使用的所有化合物均作为与底物4 - NPA的竞争性抑制剂。尿嘧啶衍生物是新兴的碳酸酐酶抑制剂,可用于生物医学。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/2425/6009904/7b24cd465d49/IENZ_A_1235043_F0001_B.jpg

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