An entry from the Cambridge Structural Database, the world’s repository for small molecule crystal structures. The entry contains experimental data from a crystal diffraction study. The deposited dataset for this entry is freely available from the CCDC and typically includes 3D coordinates, cell parameters, space group, experimental conditions and quality measures.
Objective
To investigate the distribution and drug resistance of pathogens isolated from the critical patients with ventilator-associated infections in ICU from our hospital.
Methods
561 critically ill patients treated by mechanical ventilation from January, 2016 to December, 2017 in the ICU of our hospital were selected. 65 sputum specimens from the patients with ventilator related infection were collected, and the bacteria were cultured and isolated. The bacterial identification and drug sensitivity test were carried out by VITEK 2-Compact automatic bacterial identification instrument, and the results were statistically analyzed by WHONET5.6.
Results
Among the 65 patients with ventilator-associated infection, 101 strains of pathogenic bacteria were cultured. There were 71 strains of negative bacteria, accounting for 70.30%; 9 strains of positive bacteria, accounting for 8.91%; and 21 strains of fungi, accounting for 20.79%. Among the gram-negative bacilli, the top three pathogenic bacteria were 22 strains of acinetobacter bauman, accounting for 21.78%; 20 strains of pseudomonas aeruginosa, accounting for 19.80%; and 12 strains of klebsiella pneumoniae, accounting for 11.89%. The 9 strains of Gram-positive bacteria were staphylococcus aureus. The drug sensitivity results showed that the proportion of carbapenem resistant acinetobacter bauman (CRABA) was 95.2%, the proportion of carbapenem resistant pseudomonas aeruginosa (CRPAE) was 28.6%, and the proportion of methicillin resistant staphylococcus aureus (MRSA) was 100.0%.
Conclusion
The pathogenic bacteria associated with ventilator related infection in critically ill patients in the ICU in our hospital are mainly Gram-negative bacteria; the proportions of MRSA, CRABA, and CRPAE are very high, which brings severe test to clinical treatment. It is necessary to take corresponding countermeasures to control drug resistant bacteria.
Key words:
Critically ill patients in ICU; Ventilator associated infection; Pathogens; Drug resistance
Objective To explore the antimicrobial resistance of Acinetobacter baumannii and the genotype of multidrug-resistant β-Lactamase producing Acinetobacter baumannii isolated from clinical specimens in order to provide the laboratory information for effective control and treatment of the infectious diseases.Method Kirby-Bauer(K-B) tests were performed to detect the susceptibility of 312 strains of Acinetobacter baumannii to 13 kinds of antimicrobial agents.The genotypes of β-Lactamase producing gene in multidrug-resistant Acometobacter baumannii were detected by multiple PCR amplification and then the DNA products were sequenced.Result The resistance rates of the 312 Acinetobacter baumannii isolates to Imipenam,Cefoperazone/sulbactam and Ticarcillin/clavulanic were 1.0%,30.8% and 31.4%,respectively.The resistance rates to other antimicrobial agents were between 38.5%～80.1%.The positive rates of AmpC,SHV-12,PER-1,CTX-M-9 and TEM-1 among β-Lactamase genes in 120 multidrug-resistant strains were 66.7%(80/120),14.2%(17/120),16.7%(20/120),8.2%(10/120) and 9.2% (11/120),respectively.VER-1,CTX-M-1,CTX-M-2 and OXA genes were not found.There were two different genes in 16 strains,and three different genes in 14 strains.Conclusion Strains that produce AmpC were predominant among Acinetobacter baumannii isolated from clinical specimens and were also multiresistant.
There are numerous published studies establishing a link between reactive metabolite formation and toxicity of various drugs. Although the correlation between idiosyncratic reactions and reactive metabolite formation is not 1:1, the association between the two is such that many pharmaceutical companies now monitor for reactive metabolites as a standard part of drug candidate testing and selection. The most common method involves in vitro human microsomal incubations in the presence of a thiol trapping agent, such as glutathione (GSH), followed by LC/MS analysis. In this study, we describe several 2,7-disubstituted-pyrrolotriazine analogues that are extremely potent reactive metabolite precursors. Utilizing a UPLC/UV/MS method, unprecedented levels of GSH adducts were measured that are 5–10 times higher than previously reported for high reactive metabolite-forming compounds such as clozapine and troglitazone.
A novel 2,7-disubstituted-pyrrolo[2,1-f][1,2,4]triazine scaffold has been designed as a new kinase inhibitor platform mimicking the bioactive conformation of the well-known diaminopyrimidine motif. The design, synthesis, and validation of this new pyrrolo[2,1-f][1,2,4]triazine scaffold will be described for inhibitors of anaplastic lymphoma kinase (ALK). Importantly, incorporation of appropriate potency and selectivity determinants has led to the discovery of several advanced leads that were orally efficacious in animal models of anaplastic large cell lymphoma (ALCL). A lead inhibitor (30) displaying superior efficacy was identified and in depth in vitro/in vivo characterization will be presented.
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