Schistosomiasis is considered a serious public health problem in 78 countries and territories located in Africa, Asia and America and it is estimated in more than 249 million people infected by any of the species of Schistosoma. The exclusive use of praziquantel (PZQ), effective drug against all species of Schistosoma, has been the basis of the development of a possible resistance against the strains of this parasite. In addition, PZQ is not effective against young forms of worms. Thus, there is a need for the development of new drugs with schistosomicidal activity. The objective of this work was to synthesize and to evaluate the therapeutic potential of new benzodioxole derivatives (3–14) candidates for schistosomicidal drugs. All compounds synthesized showed in vitro schistosomicidal activity. The derivative 12 was considered the best compound, since it took 100% of worms to mortality in the first 72 h of exposure at the concentration of 100 μM and 83.3% at the concentration of 50 μM. Furthermore, male and female adult worms, incubated for 24 h with the compound 12 showed tegument damages characterized by extensive desquamation and edema, tuber destruction, bubble formation and exposure of the muscle layer. This compound has a restricted structure, where the thiazolidinone is attached to the 4-position of the 1,3-benzodioxol ring. The structural conformation of derivative 12 was probably responsible for the promising schistosomicidal activity, where the presence of an electron/conformational restriction of the thiazolidine ring, as well as the action of bromine as a bulk substitute, favored an increase in biological activity. In addition, tegumentary changes caused by derivative 12 may also have been responsible for the death of adult worms of Schistosoma mansoni. Therefore, we verified that the results obtained in this study make benzodioxole derivatives possible candidates for prototypes of new schistosomicidal drugs.

在非洲，亚洲和美洲的78个国家和地区，血吸虫病被认为是严重的公共卫生问题，估计有2.49亿人感染了任何一种血吸虫病。吡喹酮（PZQ）（一种针对所有血吸虫的有效药物）的独家使用，已成为对这种寄生虫菌株产生抗药性的基础。另外，PZQ对年轻形式的蠕虫无效。因此，需要开发具有血吸虫杀伤活性的新药。这项工作的目的是合成和评估新的苯并二恶唑衍生物的治疗潜力（3–14）血吸虫药的候选人。合成的所有化合物均显示出体外血吸虫杀虫活性。衍生物12被认为是最好的化合物，因为在暴露的头72小时内，浓度为100μM的蠕虫的死亡率为100％，浓度为50μM的蠕虫的死亡率为83.3％。此外，与化合物12一起温育24小时的成年和成年雌性蠕虫显示出皮被损害，其特征在于广泛的脱皮和浮肿，块茎破坏，气泡形成和肌肉层暴露。该化合物具有受限的结构，其中噻唑烷酮连接至1,3-苯并二恶唑环的4位。衍生物12的结构构象可能是有希望的血吸虫杀虫活性的原因，其中噻唑烷环的电子/构象限制以及溴作为主体替代物的作用促进了生物活性的提高。此外，由导数12引起的表皮变化也可能是造成曼氏血吸虫成虫的死亡的原因。因此，我们验证了本研究中获得的结果使苯并二恶唑衍生物可能成为新的血吸虫杀虫剂原型的候选者。