关键词: Pseudomonas aeruginosa biofilm c-di-GMP dispersal dust analysis flow chemistry large-scale synthesis preclinical pyrazole safety

Mesh : Pyrazoles / chemistry pharmacology chemical synthesis Pseudomonas aeruginosa / drug effects Anti-Bacterial Agents / pharmacology chemical synthesis chemistry Biofilms / drug effects Humans Pseudomonas Infections / drug therapy microbiology Risk Assessment

来  源:   DOI:10.3390/ijms25126737   PDF(Pubmed)

Abstract:
This paper presents the work performed to transition a lab-scale synthesis (1 g) to a large-scale (400 g) synthesis of the 3-5-diamino-1H-Pyrazole Disperazol, a new pharmaceutical for treatment of antibiotic-resistant Pseudomonas aeruginosa biofilm infections. The potentially hazardous diazotisation step in the lab-scale synthesis was transformed to a safe and easy-to-handle flow chemistry step. Additionally, the paper presents an OSHA-recommended safety assessment of active compound E, as performed by Fauske and Associates, LLC, Burr Ridge, IL, USA.
摘要:
本文介绍了将实验室规模的合成(1g)过渡到大规模(400g)合成3-5-二氨基-1H-吡唑的工作。一种治疗抗生素耐药铜绿假单胞菌生物膜感染的新药。将实验室规模合成中潜在危险的重氮化步骤转变为安全且易于处理的流动化学步骤。此外,本文介绍了OSHA推荐的活性化合物E的安全性评估,由Fauske和Associates表演,LLC,伯尔岭,IL,美国。
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