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Research Paper

Synthesis and biological evaluation of aminomethyl and alkoxymethyl derivatives as carbonic anhydrase, acetylcholinesterase and butyrylcholinesterase inhibitors

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Pages 1174-1182 | Received 21 Mar 2017, Accepted 13 Aug 2017, Published online: 11 Sep 2017

Figures & data

Figure 1. The hydrolyze reaction of acetylcholine in the presence of acetylcholinesterase enzyme (AChE).

Figure 1. The hydrolyze reaction of acetylcholine in the presence of acetylcholinesterase enzyme (AChE).

Table 1. Physico-chemical characteristics of aminomethyl derivatives of benzothiazol- and benzoxazolthiones

Table 2. Physico-chemical characteristics of the alkoxymethyl derivatives of benzoxazolthione and 2-aminothiazoles.

Table 3. AChE, human carbonic anhydrase I, and II isoforms (hCA I, and II) AChE and BChE enzymes inhibition effects of aminomethyl and alkoxymethyl derivatives (1–17) and proportion of AChE to BChE enzymes.

Figure 2. (a) IC50 values of aminomethyl and alkoxymethyl derivatives for hCA I, and II isoenzymes. (b) IC50 values of aminomethyl and alkoxymethyl derivatives for AChE and BChE enzymes. (c) Ki values of aminomethyl and alkoxymethyl derivatives for hCA I, and II isoenzymes. (d) Ki values of aminomethyl and alkoxymethyl derivatives for AChE and BChE enzymes.

Figure 2. (a) IC50 values of aminomethyl and alkoxymethyl derivatives for hCA I, and II isoenzymes. (b) IC50 values of aminomethyl and alkoxymethyl derivatives for AChE and BChE enzymes. (c) Ki values of aminomethyl and alkoxymethyl derivatives for hCA I, and II isoenzymes. (d) Ki values of aminomethyl and alkoxymethyl derivatives for AChE and BChE enzymes.