当前位置：
X-MOL 学术
›
ChemMedChem
›
论文详情
Our official English website, www.x-mol.net, welcomes your
feedback! (Note: you will need to create a separate account there.)
Synthesis, Design, and Structure-Activity Relationship of a Benzenesulfonylpiperazine Series against Trypanosoma cruzi
ChemMedChem ( IF 3.6 ) Pub Date : 2022-08-22 , DOI: 10.1002/cmdc.202200211 Ana Clara Cassiano Martinho 1 , Daniela de Melo Resende 2 , Emanuelly Silva Landin 1 , Thibault Joseph William Jacques Dit Lapierre 1 , Talita Cristina Diniz Bernardes 3 , Luan Carvalho Martins 3 , Rafaela Salgado Ferreira 3 , Silvane Maria Fonseca Murta 2 , Celso de Oliveira Rezende Júnior 1
ChemMedChem ( IF 3.6 ) Pub Date : 2022-08-22 , DOI: 10.1002/cmdc.202200211 Ana Clara Cassiano Martinho 1 , Daniela de Melo Resende 2 , Emanuelly Silva Landin 1 , Thibault Joseph William Jacques Dit Lapierre 1 , Talita Cristina Diniz Bernardes 3 , Luan Carvalho Martins 3 , Rafaela Salgado Ferreira 3 , Silvane Maria Fonseca Murta 2 , Celso de Oliveira Rezende Júnior 1
Affiliation
|
An early hit-to-lead optimization process of a novel benzenesulfonylpiperazine series against Trypanosoma cruzi was started. Synthesis, design, biological evaluation, and SAR study were performed, and compounds with good levels of potency (IC50 ∼5 μM), selectivity (>50) and a promising predicted ADMET profile were identified, being candidates for further development towards therapies for Chagas disease.
中文翻译：
苯磺酰哌嗪系列抗克氏锥虫的合成、设计及构效关系
开始了针对克氏锥虫的新型苯磺酰基哌嗪系列的早期命中至先导优化过程。进行了合成、设计、生物学评价和 SAR 研究，并确定了具有良好效力水平 (IC 50 ∼ 5 μM)、选择性 (>50) 和有希望的预测 ADMET 特征的化合物，作为进一步开发治疗药物的候选者南美锥虫病。
更新日期：2022-08-22
中文翻译：
苯磺酰哌嗪系列抗克氏锥虫的合成、设计及构效关系
开始了针对克氏锥虫的新型苯磺酰基哌嗪系列的早期命中至先导优化过程。进行了合成、设计、生物学评价和 SAR 研究，并确定了具有良好效力水平 (IC 50 ∼ 5 μM)、选择性 (>50) 和有希望的预测 ADMET 特征的化合物，作为进一步开发治疗药物的候选者南美锥虫病。
京公网安备 11010802027423号