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Livio Racané, Lucija Ptiček, Mirela Sedić, Petra Grbčić, Sandra Kraljević Pavelić, Branimir Bertoša, Irena Sović, Grace Karminski-Zamola
Herein, we describe the synthesis of twenty-one novel water-soluble monocationic 2-aryl/heteroaryl-substituted 6-(2-imidazolinyl)benzothiazole mesylates 3a-3u and present the results of their anti-proliferative assays. Efficient syntheses were achieved by three complementary simple two-step synthetic protocols based on the condensation reaction of aryl/heteroaryl carbaldehydes or carboxylic acid. We developed an eco-friendly synthetic protocol using glycerol as green solvent, particularly appropriate for the condensation of thermally and acid-sensitive heterocycles such as furan, benzofuran, pyrrole, and indole...
April 17, 2018: Molecular Diversity
Yongda Zhao, Lili Guo, Jie Li, Xianhui Huang, Binghu Fang
Background: Haemophilus parasuis is a common porcine respiratory pathogen that causes high rates of morbidity and mortality in farmed swine. We performed a molecular characterization of antimicrobial resistance genes harbored by H. parasuis from pig farms in China. Methods: We screened 143 H. parasuis isolates for antimicrobial susceptibility against six fluoroquinolone antibiotics testing by the broth microdilution method, and the presence of 64 antimicrobial resistance genes by PCR amplification and DNA sequence analysis...
2018: PeerJ
Yingying Shao, Pin Zhao, Qinyan Yue, Yuwei Wu, Baoyu Gao, Wenjia Kong
Wheat straw-supported Nanoscale Zero-Valent Iron particles (WS-NZVI) were successfully synthesized, which were used for Ciprofloxacin hydrochloride (CIP) removal in simulation wastewater. The structure, chemical composition and micro-morphology of WS-NZVI and Nanoscale Zero-Valent Iron (NZVI) were characterized by scanning electron microscopy analysis (SEM), X-ray diffraction (XRD), as well as the Fourier Transformed IR spectra (FT-IR). XRD results proved the existence of Fe°, and SEM images indicated that the agglomeration of NZVI was effectively inhibited when loaded on wheat straw...
April 14, 2018: Ecotoxicology and Environmental Safety
Xi Li, Long Sun, Yongze Zhu, Mengyuan Shen, Yuexing Tu
OBJECTIVES: The emergence of Carbapenem-resistant E. coli has become a serious challenge to manage in the clinic because of multi-drug resistance. Here, we report the draft genome sequence of a NDM-3-producing E. coli strain NT1 that was isolated from bloodstream infection in China. METHODS: Whole-genomic DNA of E. coli strain NT1 was extracted and was sequenced using an Illumina-Hiseq™ X Ten platform. The generated sequence reads were assembled using CLC Genomics Workbench...
April 14, 2018: Journal of Global Antimicrobial Resistance
Tyrell R Towle, Chaitanya A Kulkarni, Lisa M Oppegard, Bridget P Williams, Taylor A Picha, Hiroshi Hiasa, Robert J Kerns
Structural studies of topoisomerase-fluoroquinolone-DNA ternary complexes revealed a cavity between the quinolone N-1 position and the active site tyrosine. Fluoroquinolone derivatives having positively charged or aromatic moieties extended from the N-1 position were designed to probe for binding contacts with the phosphotyrosine residue in ternary complex. While alkylamine, alkylphthalimide, and alkylphenyl groups introduced at the N-1 position afforded derivatives that maintained modest inhibition of the supercoiling activity of DNA gyrase, none retained ability to poison DNA gyrase...
March 30, 2018: Bioorganic & Medicinal Chemistry Letters
B J A Berendsen, J Lahr, C Nibbeling, L J M Jansen, I E A Bongers, E L Wipfler, M G M van de Schans
After administration to livestock, a large fraction of antibiotics are excreted unchanged via excreta and can be transferred to agricultural land. For effective risk assessment a critical factor is to determine which antibiotics can be expected in the different environmental compartments. After excretion, the first relevant compartment is manure storage. In the current study, the fate of a broad scope of antibiotics (n = 46) during manure storage of different livestock animals (calves, pigs, broilers) was investigated...
April 11, 2018: Chemosphere
Ursula Fürnkranz, Julia Walochnik, Birgit Henrich
OBJECTIVES: Mycoplasma hominis, a genetically heterogeneous, cell-wall less bacterium, is able to live in symbiosis with the protozoan parasite Trichomonas vaginalis. While impacts of this symbiosis on T. vaginalis have been investigated to a certain extent, less light has been shed on the influence on M. hominis. METHODS: In an in vitro minimal inhibitory concentration (MIC) study the antibiotic susceptibility of three clinical M. hominis isolates, V475, AKH136 and MhSS10, to clindamycin, moxifloxacin, ciprofloxacin and gentamicin was investigated in dependence on symbiosis with T...
April 13, 2018: Journal of Global Antimicrobial Resistance
Nicholas J Mercuro, Rachel M Kenney, Odaliz-Abreu Lanfranco, Susan L Davis
No abstract text is available yet for this article.
April 12, 2018: Clinical Infectious Diseases: An Official Publication of the Infectious Diseases Society of America
Yuyi Yang, Wenjuan Song, Hui Lin, Weibo Wang, Linna Du, Wei Xing
Lakes are an important source of freshwater, containing nearly 90% of the liquid surface fresh water worldwide. Long retention times in lakes mean pollutants from discharges slowly circulate around the lakes and may lead to high ecological risk for ecosystem and human health. In recent decades, antibiotics and antibiotic resistance genes (ARGs) have been regarded as emerging pollutants. The occurrence and distribution of antibiotics and ARGs in global freshwater lakes are summarized to show the pollution level of antibiotics and ARGs and to identify some of the potential risks to ecosystem and human health...
April 10, 2018: Environment International
Łukasz Mąka, Elżbieta Maćkiw, Monika Stasiak, Tomasz Wołkowicz, Joanna Kowalska, Jacek Postupolski, Magdalena Popowska
Distribution of amino acid substitutions in the quinolone resistance-determining region (QRDR) of gyrA, gyrB, parC, parE and determinants of plasmid-mediated quinolone resistance (PMQR) were investigated among quinolone-resistant Salmonella spp. strains isolated from retail food in Poland in the years 2008-2013. Ten different amino acid substitutions were identified in QRDRs. Five different amino acid substitutions were identified in gyrA: Ser83Tyr, Ser83Phe, Asp87Tyr, Asp87Asn, Asp87Gly, two amino acid substitutions in parC: Thr57Ser, Ser80Ile and in parE: Leu445Phe, Arg511Ser...
March 17, 2018: International Journal of Food Microbiology
Igor V Ukrainets, Lyudmila V Sidorenko, Mykola Y Golik, Igor M Chernenok, Lina A Grinevich, Alexandra A Davidenko
Continuing a targeted search for new leading structures with diuretic action among tricyclic derivatives of hydroxyquinolines, which are of interest as potential inhibitors of aldosterone synthase, the synthesis of a series of the corresponding pyrido[3,2,1- ij ]quinoline-6-carboxanilides was carried out by amidation of ethyl-7-hydroxy-5-oxo-2,3-dihydro-1 H ,5 H -pyrido[3,2,1- ij ]quinoline-6-carboxylate with aniline, aminophenols and O -alkylsubstituted analogs with high yields and purity. The optimal conditions of this reaction are proposed; they make it possible to prevent partial destruction of the original heterocyclic ester and thereby avoid formation of specific impurities of 7-hydroxy-2,3-dihydro-1 H ,5 H -pyrido[3,2,1- ij ]quinolin-5-one...
April 9, 2018: Scientia Pharmaceutica
Arnaud Gutierrez, Jonathan M Stokes, Ivan Matic
The maintenance of DNA supercoiling is essential for the proper regulation of a plethora of biological processes. As a consequence of this mode of regulation, ahead of the replication fork, DNA replication machinery is prone to introducing supercoiled regions into the DNA double helix. Resolution of DNA supercoiling is essential to maintain DNA replication rates that are amenable to life. This resolution is handled by evolutionarily conserved enzymes known as topoisomerases. The activity of topoisomerases is essential, and therefore constitutes a prime candidate for targeting by antibiotics...
April 8, 2018: Antibiotics
Yinfang Shen, Jiehao Cai, Mark R Davies, Chi Zhang, Kun Gao, Dan Qiao, Haoqin Jiang, Weilei Yao, Yuefang Li, Mei Zeng, Mingliang Chen
Streptococcus pyogenes , also known as group A Streptococcus (GAS), is one of the top 10 infectious causes of death worldwide. Macrolide and tetracycline resistant GAS has emerged as a major health concern in China coinciding with an ongoing scarlet fever epidemic. Furthermore, increasing rates of fluoroquinolone (FQ) non-susceptibility within GAS from geographical regions outside of China has also been reported. Fluoroquinolones are the third most commonly prescribed antibiotic in China and is an therapeutic alternative for multi-drug resistant GAS...
2018: Frontiers in Microbiology
Takashi Deguchi, Kyoko Hatazaki, Shin Ito, Hiromi Kondo, Kengo Horie, Keita Nakane, Kosuke Mizutani, Tomohiro Tsuchiya, Mitsuru Yasuda, Shigeaki Yokoi, Masahiro Nakano
We analyzed the 23S rRNA, gyrA and parC genes of Chlamydia trachomatis DNAs from men with urethritis and determined microbiological outcomes of an extended-release azithromycin (azithromycin-SR) regimen (2 g once daily for 1 day) and a sitafloxacin regimen (100 mg twice daily for 7 days) for chlamydial urethritis to clarify the macrolide and fluoroquinolone resistance status of clinical strains of C. trachomatis. We amplified the portions of 2 alleles of the 23S rRNA gene and the gyrA and parC genes from C...
April 4, 2018: Journal of Infection and Chemotherapy: Official Journal of the Japan Society of Chemotherapy
Yong Chong, Shinji Shimoda, Nobuyuki Shimono
The worldwide spread of extended-spectrum β-lactamase (ESBL)-producing bacteria, particularly Escherichia coli and Klebsiella pneumoniae, is a critical concern for the development of therapies against multidrug-resistant bacteria. Since the 2000s, detection rates of CTX-M types ESBL-producing E. coli in the community have been high, possibly contributing to their nosocomial detection. Various factors, such as environmental sources, food animals, and international travel, accelerate the global ESBL spread in the community...
April 4, 2018: Infection, Genetics and Evolution
Yao Sun, Hong Lu, Xiaoxiao Zhang, Qing Wu, Wenzi Bi, Haiyang Liu, Jianming Cao, Tieli Zhou
The current worldwide emergence of resistance to antibiotics in bacteria constitutes an important growing public health threat. The mechanisms of the emergence and dissemination of resistance remain to be elucidated. Adaptation laboratory evolution provide an approach to investigate the acquisition of de novo mutations that confers drug resistance. In our study, 3 Enterococcus faecalis clinical isolates and E. faecalis ATCC29212 were evolved resistant to 8 kinds of antimicrobials spanning five chemical classes, including ciprofloxacin, levofloxacin, gatifloxacin, penicillin, imipenem, vancomycin, chloramphenicol and gentamicin...
April 3, 2018: Infection, Genetics and Evolution
Rasha M Hassan, Ali M Yehia, Ola A Saleh, Aida A El-Azzouny, Hassan Y Aboul-Enein
Fluoroquinolones are popular class of antibiotics with distinct chemical functionality. Most of them are ampholytes with one chiral center. Stereogeneic center is located either in the side ring of Gatifloxacin (GFLX) or in the quinolone core of Ofloxacin (OFLX). These two amphoteric fluoroquinolones have terminal amino groups in common. The unusual Nadifloxacin (NFLX) is an acidic fluoroquinolone with a core chiral center. Owing to chirality and functionality differences among GFLX, OFLX, and NFLX, we mapped these enantiomers onto structure-retention relationship...
April 6, 2018: Chirality
Sage J B Dunham, Joseph F Ellis, Nameera F Baig, Nydia Morales-Soto, Tianyuan Cao, Joshua D Shrout, Paul W Bohn, Jonathan V Sweedler
After several decades of widespread use for mapping elemental ions and small molecular fragments in surface science, secondary ion mass spectrometry (SIMS) has emerged as a powerful analytical tool for molecular imaging in biology. SIMS has primarily been used as a qualitative technique; although the distribution of a single analyte can be accurately determined, it is difficult to map the absolute quantity of a compound, or even to compare the relative abundance of one molecular species to that of another. We describe a method for quantitative SIMS imaging of small molecules in agar-based microbial communities...
April 6, 2018: Analytical Chemistry
Juan Li, Xueling Ren, Yanyan Diao, Yu Chen, Qingli Wang, Wenting Jin, Piao Zhou, Qiqi Fan, Yanbing Zhang, Hongmin Liu
The aim of this work was to develop a simple and rapid analytical method for the simultaneous determination of a wide range of drug residues in milk by UHPLC-MS/MS. A total of 25 typical veterinary drugs investigated belong to six families including β-lactams, quinolones, β-agonists, phenicols, glucocorticoids and nitrofurans. The samples were extracted by acetonitrile and defatted with n-hexane twice. Electrospray ionization and positive/negative polarity switching were utilized for the analysis of 25 veterinary drugs in a single chromatographic run...
August 15, 2018: Food Chemistry
Jessica Petri, Yosuke Shimaki, Wanting Jiao, Hannah R Bridges, Euan R Russell, Emily J Parker, David Aragão, Gregory M Cook, Yoshio Nakatani
Type II NADH:quinone oxidoreductase (NDH-2) is a proposed drug-target of major pathogenic microorganisms such as Mycobacterium tuberculosis and Plasmodium falciparum. Many NDH-2 inhibitors have been identified, but rational drug development is impeded by the lack of information regarding their mode of action and associated inhibitor-bound NDH-2 structure. We have determined the crystal structure of NDH-2 complexed with a quinolone inhibitor 2-heptyl-4-hydroxyquinoline-N-oxide (HQNO). HQNO is nested into the slot-shaped tunnel of the Q-site, in which the quinone-head group is clamped by Q317 and I379 residues, and hydrogen-bonds to FAD...
April 2, 2018: Biochimica et Biophysica Acta
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