a Department of Chemistry, Faculty of Arts and Sciences , İnönü University , Malatya , Turkey.
b Department of Basic Pharmaceutical Sciences, Faculty of Pharmacy , İnönü University , Malatya , Turkey.
J Enzyme Inhib Med Chem. 2019 Dec;34(1):343-349. doi: 10.1080/14756366.2018.1553040.
Thirteen novel benzothiazole derivatives incorporating glycine, methionine, alanine, and phenylalanine were synthesised by facile acylation reactions through benzotriazole or DCC mediated reactions and their structures were identified by H-NMR, 13C-NMR, and FT-IR spectroscopic techniques and elemental analysis. The carbonic anhydrase (CA, EC 4.2.1.1) inhibitory activity of the new compounds was assessed against four human (h) isoforms, hCA I, hCA II, hCA V, and hCA XIII. Some of the synthesised compounds showed good in vitro carbonic anhydrase inhibitory properties, with inhibition constants in the micromolar level. The new amino acid benzothiazole conjugates found to be more effective against hCA V and hCA II inhibition. In vitro antioxidant activities of the novel compounds were determined by DPPH method. Most of the synthesised compounds showed moderate to low antioxidant activities compared to the control antioxidant compounds (BHA and α-tocopherol).
合成了 13 种新型苯并噻唑衍生物，这些衍生物通过苯并三唑或 DCC 介导的反应，通过简便的酰化反应合成，其结构通过 H-NMR、13C-NMR 和 FT-IR 光谱技术以及元素分析进行鉴定。评估了新化合物对四种人（h）同工酶（hCA I、hCA II、hCA V 和 hCA XIII）的碳酸酐酶（CA，EC 4.2.1.1）抑制活性。一些合成的化合物表现出良好的体外碳酸酐酶抑制特性，其抑制常数在微摩尔级。新的氨基酸苯并噻唑缀合物被发现对 hCA V 和 hCA II 的抑制更有效。通过 DPPH 法测定了新化合物的体外抗氧化活性。与对照抗氧化化合物（BHA 和 α-生育酚）相比，大多数合成的化合物表现出中等至低的抗氧化活性。
