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Archives of Physiology and Biochemistry
The Journal of Metabolic Diseases
Volume 124, 2018 - Issue 1
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Original Article

Synthesis of chalcone-imide derivatives and investigation of their anticancer and antimicrobial activities, carbonic anhydrase and acetylcholinesterase enzymes inhibition profiles

, , , , , , ORCID Icon & show all
Pages 61-68 | Received 18 Jul 2017, Accepted 25 Jul 2017, Published online: 09 Aug 2017
 

Abstract

The new 1-(4-(3-(aryl)acryloyl)phenyl)-1H-pyrrole-2,5-diones (5ag) were prepared from 4′-aminchalcones (3ag) and screened for biological activities. All compounds (3ag and 5ag), except 3d and 3e displayed good cytotoxic activities with IC50 values in the range of 7.06–67.46 μM. IC50 value of 5-fluorouracil (5-FU) was 90.36 μM. Moreover, most of compounds 5ag 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.

Disclosure statement

The authors declare that no conflicts of interest.

Additional information

Funding

Scientific and Technological Research Council of Turkey10.13039/501100004410111T990
The authors are indebted to the Scientific and Technological Research Council of Turkey [TUBİTAK Project No. 111T990] for financial supports.

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