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恩西芬群及其中间体的新型合成方法及其对……的抗病原特性

Novel synthesis and anti-pathogenic properties of ensifentrine and its intermediates against .

作者信息

Sajeevan Anusree, Andrew Deepthi Joseph, Patra T Nalinikanta, Solomon Adline Princy, Dandela Rambabu

机构信息

Quorum Sensing Laboratory, Centre for Research in Infectious Diseases (CRID), School of Chemical and Biotechnology, SASTRA Deemed to be University Thanjavur India

Department of Industrial and Engineering Chemistry, Institute of Chemical Technology Bhubaneswar Odisha India.

出版信息

RSC Adv. 2025 Apr 23;15(17):13053-13063. doi: 10.1039/d5ra01722j. eCollection 2025 Apr 22.

Abstract

Chronic obstructive pulmonary disease (COPD) is a progressive respiratory disorder marked by persistent lung inflammation and airway constriction. It presents a formidable global health challenge owing to its high morbidity and mortality rates. It is often aggravated by infections from pathogens such as , a predominant pathogen that accelerates lung function deterioration and triggers frequent exacerbations. Ensifentrine (ENF) exhibits strong anti-inflammatory effects and is a selective dual inhibitor of the enzymes PDE3 and PDE4, which have been reported to be beneficial in treating COPD exacerbation. This study examined the anti-pathogenic activity of ENF against by adopting an innovative synthetic route. A series of intermediates were synthesized the novel route, optimizing the yield and integrity of ENF. Further investigations to determine the activity of the compound against involved antibacterial and antibiofilm testing and identification of the potential mechanisms of action. Preliminary results demonstrate that ENF and its intermediate ENF exhibit 50-60% robust biofilm-inhibition and biofilm-eradication effects at remarkably low concentrations of 3.9 μM and 7.9 μM, respectively. Furthermore, ENF disrupts quorum sensing, leading to a 35% reduction in the production of pyoverdine and exopolysaccharide, which are two key virulence factors of . Importantly, ENF exhibits synergistic activity with ciprofloxacin, further enhancing its antimicrobial efficacy at a concentration of 0.25 μg mL. This study focuses on the innovative synthesis of ENF and its promising anti-pathogenic properties, which may make it an effective adjunctive treatment for COPD caused by .

摘要

慢性阻塞性肺疾病(COPD)是一种进行性呼吸系统疾病,其特征为持续的肺部炎症和气道狭窄。由于其高发病率和死亡率,它对全球健康构成了严峻挑战。它常常因诸如[病原体名称缺失]等病原体感染而加重,[病原体名称缺失]是一种主要病原体,会加速肺功能恶化并引发频繁发作。恩西芬净(ENF)具有强大的抗炎作用,是磷酸二酯酶3(PDE3)和磷酸二酯酶4(PDE4)的选择性双重抑制剂,据报道这两种酶在治疗COPD发作方面具有益处。本研究通过采用创新的合成路线,研究了ENF对[病原体名称缺失]的抗病原体活性。通过该新路线合成了一系列中间体,优化了ENF的产率和完整性。进一步研究该化合物对[病原体名称缺失]的活性,包括抗菌和抗生物膜测试以及确定潜在的作用机制。初步结果表明,ENF及其中间体在低至3.9 μM和7.9 μM的浓度下分别表现出50 - 60%强大的生物膜抑制和生物膜根除作用。此外,ENF破坏群体感应,导致绿脓菌素和胞外多糖的产生减少35%,这两种物质是[病原体名称缺失]的两个关键毒力因子。重要的是,ENF与环丙沙星具有协同活性,在浓度为0.25 μg/mL时进一步增强了其抗菌效果。本研究重点关注ENF的创新合成及其有前景的抗病原体特性,这可能使其成为治疗由[病原体名称缺失]引起的COPD的有效辅助治疗药物。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/c7a2/12015936/7d9d4ff16444/d5ra01722j-f1.jpg

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