An efficient, one-pot and four-component synthesis of a new series of 2,3-disubstituted isoindolin-1-ones is described and their Jack bean urease inhibitory activities are evaluated. Heating a mixture of 1,1-bis(methylthio)-2-nitroethene, a 1,2-diamine, a 2-formylbenzoic acid and a primary amine in EtOH for 3.5 h afforded the corresponding 2,3-disubstituted isoindolin-1-ones in good to excellent yields. All sixteen synthesized isoindolin-1-one derivatives 5a–p showed urease inhibitory activity. Among them, 5c showed the most urease inhibitory activity (IC₅₀ = 10.07 ± 0.28 µM) being over 2-fold more potent than thiourea (IC₅₀ = 22.01 ± 0.10 µM) and 10-fold than hydroxyurea (IC₅₀ = 100.00 ± 0.02 µM) as the standard inhibitors, respectively. Also, results from molecular docking studies were in good agreement with those obtained from in vitro tests.

描述了一个有效的，一锅和四个组成部分的新系列的新的2,3-二取代的异吲哚啉-1-酮的合成，并评估了其对Jack bean脲酶的抑制活性。将1，1-双（甲硫基）-2-硝基乙烯，1，2-二胺，2-甲酰基苯甲酸和伯胺的混合物在EtOH中加热3.5小时，得到相应的2，3-二取代的异吲哚啉-1-产量高到极好的品种。所有16种合成的异吲哚啉-1-酮衍生物5a-p均显示出脲酶抑制活性。其中5c表现出最大的脲酶抑制活性（IC ₅₀  = 10.07±0.28 µM），其效力是硫脲（IC ₅₀  = 22.01±0.10 µM）的2倍以上，是羟基脲（IC _50的10倍） = 100.00±0.02 µM）分别作为标准抑制剂。而且，分子对接研究的结果与体外测试的结果吻合良好。