Sulfonylamidine-substituted derivatives of avibactam: Synthesis and antibacterial activity,Journal of Heterocyclic Chemistry

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Sulfonylamidine-substituted derivatives of avibactam: Synthesis and antibacterial activity
Journal of Heterocyclic Chemistry ( IF 2.0 ) Pub Date : 2021-09-10 , DOI: 10.1002/jhet.4360
Jingwen Ji ₁ , Lijuan Zhai ₁ , Jian Sun ₁ , Lili He ₁ , Jinbo Ji ₁ , Xueqin Ma ₂ , Yuanbai Liu ₁ , Dong Tang ₁ , Yangxiu Mu ₁ , Yuanyu Gao ₁ , Haikang Yang ₁ , Zafar Iqbal ₁ , Zhixiang Yang ₁

Affiliation

Avibactam is a clinically approved non-β-lactam based β-lactamase inhibitor. Derivatization of this scaffold with improved inhibition profile is the demand of the day to cope with the future challenges. We successfully synthesized new derivatives of avibactam containing sulfonylamidine moieties at C2 position of the diazabicyclooctane ring. We tested in vitro antibacterial activities of newly synthesized compounds against 10 bacterial strains expressing variable β-lactamases. All compounds did not exhibit antimicrobial profile when assayed individually; however, all compounds minimized the MIC value of the imipenem in combination. Compound 5l proved most potent against all 10 bacterial strains, and showed improved inhibition against six bacterial strains as compared with the control inhibitor, relebactam. The compound 5l may be a lead hit for future development.

中文翻译：

阿维巴坦的磺酰脒取代衍生物：合成和抗菌活性

Avibactam 是一种临床批准的非β-内酰胺类β-内酰胺酶抑制剂。这种具有改进抑制特性的支架的衍生化是应对未来挑战的当今需求。我们成功地合成了在二氮杂双环辛烷环的 C2 位置含有磺酰脒部分的 avibactam 的新衍生物。我们测试了新合成化合物对 10 种表达可变 β-内酰胺酶的细菌菌株的体外抗菌活性。当单独测定时，所有化合物均未表现出抗菌特性；然而，所有化合物都使亚胺培南组合的 MIC 值最小化。化合物5l证明对所有 10 种细菌菌株最有效，并且与对照抑制剂 relebactam 相比，对 6 种细菌菌株的抑制作用有所提高。化合物5l可能是未来发展的先导。

更新日期：2021-09-10

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