Preprint Article Version 1 NOT YET PEER-REVIEWED

Discovery of Potent Carbonic Anhydrase and Acetylcholinesterase Inhibitors: 2-Aminoindan β-Lactam Derivatives

  1. Department of Chemistry, Faculty of Arts and Sciences, Sakarya University, 54050 Sakarya, Turkey
  2. Department of Basic Science, Faculty of Science, Erzurum Technical University, 25700 Erzurum, Turkey
  3. Department of Chemistry, Faculty of Sciences, İstanbul Medeniyet University, 34000 İstanbul, Turkey
  4. Department of Chemistry, Faculty of Science, Atatürk University, 25030 Erzurum, Turkey
  5. Vocational School of Health Services, Cumhuriyet University, 58140 Sivas, Turkey
  6. Department of Zoology, College of Science, King Saud University, 12364 Riyadh, Saudi Arabia
Version 1 : Received: 29 September 2016 / Approved: 30 September 2016 / Online: 30 September 2016 (05:38:45 CEST)

A peer-reviewed article of this Preprint also exists.

Genç, H.; Kalin, R.; Köksal, Z.; Sadeghian, N.; Kocyigit, U.M.; Zengin, M.; Gülçin, İ.; Özdemir, H. Discovery of Potent Carbonic Anhydrase and Acetylcholinesterase Inhibitors: 2-Aminoindan β-Lactam Derivatives. Int. J. Mol. Sci. 2016, 17, 1736. Genç, H.; Kalin, R.; Köksal, Z.; Sadeghian, N.; Kocyigit, U.M.; Zengin, M.; Gülçin, İ.; Özdemir, H. Discovery of Potent Carbonic Anhydrase and Acetylcholinesterase Inhibitors: 2-Aminoindan β-Lactam Derivatives. Int. J. Mol. Sci. 2016, 17, 1736.

Journal reference: Int. J. Mol. Sci. 2016, 17, 1736
DOI: 10.3390/ijms17101736

Abstract

β-Lactams are pharmacologically important compounds because of their various biological uses, including antibiotic and so on. β-Lactams were synthesized from benzylidene-inden derivatives and acetoxyacetyl chloride. The inhibitory effect of these compounds was also examined for human carbonic anhydrase I and II (hCA I, and II) and acetylcholinesterase (AChE). The results reveal that β-lactams are inhibitors of hCA I, II and AChE. The Ki values of β-lactams (2a-k) were 0.44-6.29 nM against hCA I, 0.93-8.34 nM against hCA II, and 0.25-1.13 nM against AChE. Our findings indicate that β-lactams (2a-k) inhibit both CA isoenzymes and AChE at low nanomolar concentrations.

Subject Areas

carbonic anhydrase; acetylcholinesterase; β-Lactam; 2-Azetidinone; enzyme inhibition; enzyme purification

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