| Summary: | Three new monosquaramides (<b>3a</b>–<b>c</b>) were synthesized, characterized by IR, NMR and X-ray, and evaluated for inhibitory activity against deoxyribonuclease I (DNase I) and xanthine oxidase (XO) in vitro. The target compounds inhibited DNase I with IC<sub>50</sub> values below 100 μM, being at the same time more potent DNase I inhibitors than crystal violet, used as a positive control. 3-Ethoxy-4-((1-(pyridin-3-yl)propan-2-yl)amino)cyclobut-3-ene-1,2-dione (<b>3c</b>) stood out as the most potent compound, exhibiting a slightly better IC<sub>50</sub> value (48.04 ± 7.98 μM) compared to the other two compounds. In order to analyze potential binding sites for the studied compounds with DNase I, a molecular docking study was performed. Compounds <b>3a</b>–<b>c</b> are among the most potent small organic DNase I inhibitors tested to date.
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