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Short Communication

Investigation of piperazines as human carbonic anhydrase I, II, IV and VII activators

, , , &
Pages 303-308 | Received 30 Nov 2017, Accepted 12 Dec 2017, Published online: 27 Dec 2017

Figures & data

Figure 1. Complex of hCA II (green, ribbon diagram, Zn(II) ion as violet sphere) with L-adrenaline, in magenta, PDB file 2HKKCitation14 and d-Trp, in yellow, PDB file 3EFICitation13b in the activator binding sites A and B, respectively. His64, in red, is shown both in its “in” and “out” conformations. The two structures were superimposed.

Figure 1. Complex of hCA II (green, ribbon diagram, Zn(II) ion as violet sphere) with L-adrenaline, in magenta, PDB file 2HKKCitation14 and d-Trp, in yellow, PDB file 3EFICitation13b in the activator binding sites A and B, respectively. His64, in red, is shown both in its “in” and “out” conformations. The two structures were superimposed.

Figure 2. 4-Aminoethyl-piperazine. A: histamine; B: piperazine; C: used as leads for the CAAs investigated in this paper.

Figure 2. 4-Aminoethyl-piperazine. A: histamine; B: piperazine; C: used as leads for the CAAs investigated in this paper.

Figure 3. Piperazines 1–24 included in the CA activation study. For the meaning of R1 and R2 see .

Figure 3. Piperazines 1–24 included in the CA activation study. For the meaning of R1 and R2 see Table 1.

Table 1. CA activation of isoforms hCA I, II, and VII (cytosolic) and IV (membrane-associated) with compounds 1-24, by a stopped-flow CO2 hydrase assayCitation21.