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目的通过设计、合成芳酰基硫脲类化合物发现新的克鲁斯氏锥体虫半胱氨酸蛋白酶小分子抑制剂。方法通过芳酰基硫代异氰酸酯和取代苯胺的反应合成芳酰基硫脲类化合物 ,化合物的结构经HRMS(EI)和1 H NMR光谱确证。结果共合成了 2 0个芳酰基硫脲类化合物 ,化合物的体外抑制克鲁斯氏锥体虫半胱氨酸蛋白酶的活性测定结果表明 :所合成的化合物均有一定的抑制克鲁斯氏锥体虫半胱氨酸蛋白酶的活性 ,其中化合物Id和In的活性高于对照药tf 175的活性。结论这类化合物有可能开发成新的抗南美锥体虫病的化疗药物
Aim To design a new aramid acyl thiourea compound for the discovery of a new inhibitor of cysteine protease small molecules. Methods The aroylthioureas were synthesized by the reaction of aroyl thioisocyanates and substituted anilines. The structures of the compounds were confirmed by HRMS (EI) and 1H NMR spectra. Results A total of 20 aroylthioureas were synthesized. The inhibitory activity of the compounds on the activity of cysteine protease of Cretaceous pyrvulina in vitro showed that the synthesized compounds all inhibited Kreu ’s cone In vivo cysteine protease activity, in which compound Id and In activity was higher than the control drug tf 175 activity. Conclusion It is possible that these compounds may be developed as new chemotherapeutic agents against S. trypanosomiasis