Qpex Biopharma, Inc., 6275 Nancy Ridge Drive, Suite 100, San Diego, California 92121, United States.
J Med Chem. 2021 Dec 9;64(23):17523-17529. doi: 10.1021/acs.jmedchem.1c01722. Epub 2021 Nov 24.
In recognition of the need for effective oral therapies to treat Gram-negative bacterial infections, efforts were directed toward identifying an oral prodrug of β-lactamase inhibitor clinical candidate QPX7728. Seventeen prodrugs were synthesized; key properties investigated were rates of cleavage to the active form in vitro, pharmacokinetics across species, and crystallinity. Compound (QPX7831 Sodium) emerged with optimal properties across all key attributes.
为了寻找有效的口服疗法来治疗革兰氏阴性菌感染，人们致力于鉴定β-内酰胺酶抑制剂临床候选药物 QPX7728 的口服前药。共合成了 17 种前药；考察的关键性质包括体外对活性形式的裂解速度、种间药代动力学和结晶度。化合物 (QPX7831 钠盐) 在所有关键属性方面均具有最佳性质。
