From DC18 to MR07: A Metabolically Stable 4,4′-Oxybisbenzoyl Amide as a Low-Nanomolar Growth Inhibitor of P. falciparum,ChemMedChem

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From DC18 to MR07: A Metabolically Stable 4,4′-Oxybisbenzoyl Amide as a Low-Nanomolar Growth Inhibitor of P. falciparum
ChemMedChem ( IF 3.6 ) Pub Date : 2022-09-11 , DOI: 10.1002/cmdc.202200355
Ivan Bassanini _{1,

2} , Silvia Parapini _{2,

3} , Nicoletta Basilico _{2,

4} , Donatella Taramelli _{2,

5} , Sergio Romeo _{2,

6}

Affiliation

Improving the metabolitc stability profile: An in silico-driven structure-activity relationship campaign (SAR) was performed to optimize the structure of a peptide decorated 4,4′-oxybisbenzoyl amide, named DC18, which showed outstanding antiplasmodial activity but poor metabolic stability in vitro. The novel lead compound, MR07, possesses low-nanomolar activity and high metabolic stability in vitro in murine and human models.

中文翻译：

从 DC18 到 MR07：代谢稳定的 4,4′-氧双苯甲酰酰胺作为恶性疟原虫的低纳摩尔生长抑制剂

改善代谢稳定性：进行了计算机驱动的结构-活性关系活动（SAR）来优化修饰的 4,4'-氧双苯甲酰酰胺的肽的结构，命名为 DC18，该肽在体内表现出出色的抗疟原虫活性，但代谢稳定性较差。体外。新型先导化合物 MR07 在体外小鼠和人类模型中具有低纳摩尔活性和高代谢稳定性。

更新日期：2022-09-11

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