a Vocational School of Health Services , Cumhuriyet University , Sivas , Turkey.
b Department of Chemistry, Faculty of Arts and Sciences , Gaziosmanpasa University , Tokat , Turkey.
Arch Physiol Biochem. 2018 Feb;124(1):61-68. doi: 10.1080/13813455.2017.1360914. Epub 2017 Aug 9.
The new 1-(4-(3-(aryl)acryloyl)phenyl)-1H-pyrrole-2,5-diones (5a-g) were prepared from 4'-aminchalcones (3a-g) and screened for biological activities. All compounds (3a-g and 5a-g), except 3d and 3e displayed good cytotoxic activities with IC values in the range of 7.06-67.46 μM. IC value of 5-fluorouracil (5-FU) was 90.36 μM. Moreover, most of compounds 5a-g showed high antibacterial activity with 8-20 mm of inhibition zone (19-25 mm of Sulbactam-Cefoperazone (SCF)). In addition, they showed good inhibitory action against acetylcholinesterase (AChE), and human carbonic anhydrase I, and II (hCA I and hCA II) isoforms. Also, these compounds demonstrated effective inhibition profiles with Ki values of 426.47-699.58 nM against hCA I, 214.92-532.21 nM against hCA II, and 70.470-229.42 nM against AChE. On the other hand, acetazolamide, clinically used drug, showed a Ki value of 977.77 ± 227.4 nM against CA I, and 904.47 ± 106.3 nM against CA II, respectively. Also, tacrine inhibited AChE showed a Ki value of 446.56 ± 58.33 nM.
新的 1-(4-(3-(芳基)丙烯酰基)苯基)-1H-吡咯-2,5-二酮（5a-g）由 4'-氨基查耳酮（3a-g）制备，并对其生物活性进行了筛选。除了 3d 和 3e 之外，所有化合物（3a-g 和 5a-g）均表现出良好的细胞毒性活性，IC 值在 7.06-67.46 μM 范围内。5-氟尿嘧啶（5-FU）的 IC 值为 90.36 μM。此外，大多数化合物 5a-g 表现出较高的抗菌活性，抑制圈为 8-20 mm（舒巴坦-头孢哌酮（SCF）为 19-25 mm）。此外，它们对乙酰胆碱酯酶（AChE）和人碳酸酐酶 I 和 II（hCA I 和 hCA II）同工酶表现出良好的抑制作用。这些化合物对 hCA I 的抑制作用Ki 值为 426.47-699.58 nM，对 hCA II 的抑制作用Ki 值为 214.92-532.21 nM，对 AChE 的抑制作用Ki 值为 70.470-229.42 nM。另一方面，临床上使用的药物乙酰唑胺对 CA I 的 Ki 值为 977.77±227.4 nM，对 CA II 的 Ki 值为 904.47±106.3 nM。此外，他克林抑制 AChE 的 Ki 值为 446.56±58.33 nM。
