Design, Synthesis, Biological Evaluation, and Molecular Docking Study of 4,6-Dimethyl-5-aryl/alkyl-2-[2-hydroxy-3-(4-substituted-1-piperazinyl)propyl]pyrrolo[3,4-<i>c</i>]pyrrole-1,3(2<i>H</i>,5<i>H</i>)-diones as Anti-Inflammatory Agents with Dual Inhibition of COX and LOX
In the present study, we characterize the biological activity of a newly designed and synthesized series of 15 compounds 2-[2-hydroxy-3-(4-substituted-1-piperazinyl)propyl] derivatives of pyrrolo[3,4-<i>c</i>]pyrrole <b>3a</b>-<b>3o</b>. The compounds were obtaine...
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| Main Authors: | , , , , , |
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| Format: | Book |
| Published: |
MDPI AG,
2023-05-01T00:00:00Z.
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| Online Access: | Connect to this object online. |
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| Summary: | In the present study, we characterize the biological activity of a newly designed and synthesized series of 15 compounds 2-[2-hydroxy-3-(4-substituted-1-piperazinyl)propyl] derivatives of pyrrolo[3,4-<i>c</i>]pyrrole <b>3a</b>-<b>3o</b>. The compounds were obtained with good yields of pyrrolo[3,4-<i>c</i>]pyrrole scaffold <b>2a</b>-<b>2c</b> with secondary amines in C<sub>2</sub>H<sub>5</sub>OH. The chemical structures of the compounds were characterized by <sup>1</sup>H-NMR, <sup>13</sup>C-NMR, FT-IR, and MS. All the new compounds were investigated for their potencies to inhibit the activity of three enzymes, i.e., COX-1, COX-2, and LOX, by a colorimetric inhibitor screening assay. In order to analyze the structural basis of interactions between the ligands and cyclooxygenase/lipooxygenase, experimental data were supported by the results of molecular docking simulations. The data indicate that all of the tested compounds influence the activity of COX-1, COX-2, and LOX. |
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| Item Description: | 10.3390/ph16060804 1424-8247 |