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In this study, a series of novel Schiff base derivatives containing a pyrazolone ring (2a-e) were designed, successfully synthesized for the first time, and characterized by elemental analysis and some spectroscopic methods. These compounds were tested for their inhibitory activities on acetylcholinesterase (AChE), butyrylcholinesterase (BChE), and the human carbonic anhydrase isoenzymes I and II (hCA I and II). All synthesized molecules indicated significant inhibition effects with IC 50 values ranging from 14.15 to 107.62 nM against these enzymes. Compound 2d showed the most potent inhibitory activity among the tested molecules toward AChE and BChE (IC 50 = 15.07 and 14.15 nM) compared to the standard drug neostigmine. We determined that the IC 50 values of the tested molecules ranged between 16.86 and 57.96 nM for hCA I and 15.24-46.21 nM for hCA II. As a consequence, we may say that some of the Schiff base derivatives may be used as potential drug candidates in later studies.

In this research, nine novel heterocyclic Schiff base derivatives (10–18) bearing an aryl sulfonate moiety were designed, synthesized for the first time, and characterized. Then, their inhibitory effects on acetyl‐ and butyrylcholinesterase (AChE and BChE) were investigated in vitro conditions. Moreover, their antioxidant activities were examined by DPPH and ABTS methods. The results indicated that some of the tested molecules had varying enzyme inhibition and antioxidant activities. We determined that compounds 8, 9, 14, 17, and 18 indicated inhibitory effects with IC50 values ranging from 89.30 to 111.28 μM against BChE, respectively compared to standard compound galanthamine (IC50 = 125.88 μM). On the other hand, of the molecules tested, only compound 5 (IC50 = 36.64 μM) displayed inhibitory activity higher than galanthamine against AChE. In DPPH assay, compounds 15 (IC50 = 161.93 μM), 16 (IC50 = 191.76 μM) and 17 (IC50 = 107.55 μM) showed higher antioxidant activity than BHT (IC50 = 203.50 μM). On the other hand, it was determined in ABTS assay that Schiff bases 10–17 (except for compound 18) indicated higher antioxidant activity than BHT.

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