Department of Chemistry, Faculty of Arts and Sciences, İnönü University, Malatya, Turkey.
Department of Basic Pharmaceutical Sciences, Faculty of Pharmacy, İnönü University, Malatya, Turkey.
J Enzyme Inhib Med Chem. 2020 Dec;35(1):1021-1026. doi: 10.1080/14756366.2020.1751620.
New dipeptide-dihydroquinolinone derivatives were successfully synthesised by benzotriazole mediated nucleophilic acyl substitution reaction and their structures were elucidated by spectroscopic and analytic techniques. The carbonic anhydrase (CA, EC 4.2.1.1) inhibitory activity of the new compounds was determined against four human (h) isoforms, hCA I, hCA II, hCA IX and hCA XII. While all compounds showed moderate to good CA inhibitory properties against hCA IX and hCA XII with inhibition constants in the micromolar level (37.7-86.8 and 2.0-8.6 µM, respectively), they did not show inhibitory activity against hCA I and hCA II up to 100 µM concentration. The antioxidant capacity of the peptide-dihydroquinolinone conjugates was determined using 1,1-diphenyl-2-picrylhydrazyl (DPPH) radical scavenging method. Most of the synthesised compounds showed low antioxidant activities compared to the control antioxidant compounds BHA and α-tocopherol.
新型二肽-二氢喹啉酮衍生物通过苯并三唑介导的亲核酰取代反应成功合成，并通过光谱和分析技术阐明了它们的结构。新化合物对四种人源（h）同工酶 hCA I、hCA II、hCA IX 和 hCA XII 的碳酸酐酶（CA，EC 4.2.1.1）抑制活性进行了测定。虽然所有化合物对 hCA IX 和 hCA XII 均表现出中等至良好的 CA 抑制特性，其抑制常数在微摩尔水平（分别为 37.7-86.8 和 2.0-8.6 μM），但它们在 100 μM 浓度下对 hCA I 和 hCA II 没有抑制活性。采用 1,1-二苯基-2-苦基肼（DPPH）自由基清除法测定了肽-二氢喹啉酮缀合物的抗氧化能力。与对照抗氧化剂 BHA 和 α-生育酚相比，大多数合成化合物的抗氧化活性较低。
