Despite the serious public health problems caused by Chagas disease in several countries, the available therapy remains with only two drugs that are poorly active during the chronic phase of the disease in addition to having severe side effects. In search of new trypanocidal agents, herein we describe the synthesis and biological evaluation of eleven new 1,6-diphenyl-1H-pyrazolo[3,4-b]pyridine compounds containing the carbohydrazide or the 2,3-dihydro-1,3,4-oxadiazole moieties. Two of them showed promising in vitro activity against amastigote forms of T. cruzi and were evaluated in vivo in male BALB/c mice infected with T. cruzi Y strain. Our results suggest that the substitution at the C-2 position of the phenyl group connected to the carbohydrazide or to the 2,3-dihydro-1,3,4-oxadiazole moieties plays an important role in the trypanocidal activity of this class of compounds. Moreover, the compound containing the 2,3-dihydro-1,3,4-oxadiazole moiety has demonstrated more favorable structural requirements for in vivo activity than its carbohydrazide analog.

尽管在一些国家由恰加斯病引起了严重的公共卫生问题，但可用的治疗方法仍然只有两种在疾病的慢性阶段活性较差且具有严重副作用的药物。为了寻找新的锥虫杀灭剂，本文描述了 11 种新的 1,6-二苯基-1 H-吡唑并[3,4- b ]吡啶化合物的合成和生物学评价，其中含有碳酰肼或 2,3-二氢-1， 3,4-恶二唑部分。其中两个对克氏锥虫的无鞭毛体形式显示出有希望的体外活性，并在感染了克氏锥虫的雄性 BALB/c 小鼠中进行了体内评估Y应变。我们的结果表明，与碳酰肼或 2,3-二氢-1,3,4-恶二唑部分相连的苯基的 C-2 位取代在此类化合物的杀锥虫活性中起着重要作用. 此外，含有 2,3-二氢-1,3,4-恶二唑部分的化合物已证明比其碳酰肼类似物对体内活性更有利的结构要求。