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Assignment of the human histone deacetylase 4 gene (HDAC4) to chromosome 2q37.2 by in situ hybridization.
U Mahlknecht et al.
Cytogenetics and cell genetics, 93(1-2), 137-138 (2001-07-28)
Jun Okuda et al.
Antimicrobial agents and chemotherapy, 54(11), 4917-4919 (2010-09-02)
A mini-Tn5 insertion into a ciprofloxacin (CIP)-resistant mutant of Vibrio cholerae O1 revealed that overexpression of the vca0421 gene, which encodes a hypothetical protein, in the CIP-resistant mutant carrying a mutation in the quinolone resistance-determining region (QRDR) of the gyrA
Masayuki Ohtsuka et al.
Antimicrobial agents and chemotherapy, 53(7), 3147-3149 (2009-05-06)
Six Bordetella pertussis strains isolated from children in Japan from 2004 to 2006 showed high-level resistance to nalidixic acid (NAL; MIC, >256 microg/ml) and decreased susceptibilities to fluoroquinolones. All of the NAL-resistant strains had the same D87G mutation in gyrA.
Manthena V S Varma et al.
Journal of medicinal chemistry, 53(3), 1098-1108 (2010-01-15)
Oral bioavailability (F) is a product of fraction absorbed (Fa), fraction escaping gut-wall elimination (Fg), and fraction escaping hepatic elimination (Fh). In this study, using a database comprised of Fa, Fg, Fh, and F values for 309 drugs in humans
Kenichiro Shimizu et al.
Antimicrobial agents and chemotherapy, 52(10), 3823-3825 (2008-07-23)
A new chromosome-carried quinolone resistance gene from Stenotrophomonas maltophilia, Smqnr, was characterized. The gene was present in type strain CCUG 5866 and was also detected in 24 clinical isolates and showed some allelic diversity. The expression of Smqnr in Escherichia
Matthew G Blango et al.
Antimicrobial agents and chemotherapy, 54(5), 1855-1863 (2010-03-17)
Numerous antibiotics have proven to be effective at ameliorating the clinical symptoms of urinary tract infections (UTIs), but recurrent and chronic infections continue to plague many individuals. Most UTIs are caused by strains of uropathogenic Escherichia coli (UPEC), which can
Longzhu Cui et al.
Antimicrobial agents and chemotherapy, 53(3), 1231-1234 (2009-01-07)
We describe here the genetic analysis of a vancomycin-susceptible Staphylococcus aureus (VSSA) strain, Mu50Omega, a strain related to vancomycin-intermediate S. aureus (VISA) strain Mu50. Using a combination of Mu50Omega whole-genome sequencing and genome engineering, we observed a stepwise evolution of
Brijesh Kumar Srivastava et al.
Bioorganic & medicinal chemistry letters, 17(7), 1924-1929 (2007-02-06)
Synthesis and antibacterial activity of a number of substituted 4,5,6,7-tetrahydro-thieno[3,2-c]pyridine quinolones is reported. The antibacterial activities were evaluated in standard in vitro MIC assay method. Some of the compounds showed in vitro (MIC) antibacterial activity comparable to those of Gatifloxacin
Vibrio splendidus as the source of plasmid-mediated QnrS-like quinolone resistance determinants.
Vincent Cattoir et al.
Antimicrobial agents and chemotherapy, 51(7), 2650-2651 (2007-04-25)
Alka Khanna et al.
Antimicrobial agents and chemotherapy, 54(11), 4789-4793 (2010-08-18)
We screened 194 Mycobacterium tuberculosis strains isolated from tuberculosis (TB) patients in Delhi and neighboring regions in India to identify the prevalence of extensive drug resistance (XDR) in clinical isolates. Among these, 104 isolates were found to be multidrug resistant
S Page et al.
Antimicrobial agents and chemotherapy, 52(11), 4155-4158 (2008-08-30)
Fluoroquinolone resistance in Streptococcus pneumoniae mainly involves stepwise mutations predominantly in the parC and gyrA genes. We have developed a single-run real-time PCR assay for detection of the four most common mutations in the quinolone resistance-determining regions of these genes.
Vincent Cattoir et al.
Antimicrobial agents and chemotherapy, 52(8), 2929-2932 (2008-06-04)
A novel QnrB-like plasmid-mediated resistance determinant, QnrB19, was identified from an Escherichia coli clinical isolate from Colombia. Its gene was associated with an ISEcp1-like insertion element that did not act as a promoter for its expression. Using an in vitro
Mohan N Patel et al.
Bioorganic & medicinal chemistry, 17(15), 5648-5655 (2009-07-08)
Here in we tried to increase an antibacterial activity of ciprofloxacin drug due to formation of mixed-ligand complexes. Synthesized compounds were found to be more potent compare to drugs, ligands and metal salt against selective gram((+ve)) and gram((-ve)) organisms. Interaction
Jenny M Pedersen et al.
Journal of medicinal chemistry, 51(11), 3275-3287 (2008-05-07)
The chemical space of registered oral drugs was explored for inhibitors of the human multidrug-resistance associated protein 2 (MRP2; ABCC2), using a data set of 191 structurally diverse drugs and drug-like compounds. The data set included a new reference set
Stéphanie Matrat et al.
Antimicrobial agents and chemotherapy, 51(5), 1643-1648 (2007-02-28)
Mycobacterium leprae, the causative agent of leprosy, is noncultivable in vitro; therefore, evaluation of antibiotic activity against M. leprae relies mainly upon the mouse footpad system, which requires at least 12 months before the results become available. We have developed
Kunikazu Yamane et al.
Antimicrobial agents and chemotherapy, 51(9), 3354-3360 (2007-06-06)
Plasmid-mediated Qnr and AAC(6')-Ib-cr have been recognized as new molecular mechanisms affecting fluoroquinolone (FQ) resistance. C316, an Escherichia coli strain demonstrating resistance to various FQs, was isolated in Japan. Resistance to FQs was augmented in an E. coli CSH2 transconjugant
Aura Rusu et al.
Journal of chromatographic science, 52(8), 919-925 (2013-08-03)
The migration behavior and separation of 13 quinolone antibacterials were investigated by capillary electrophoresis (CE). In order to predict the electrophoretic mobility, the protonation macroconstants of all the compounds were determined by pH-potentiometric titrations. We proved that the electrophoretic mobility
Lei Jia et al.
Bioorganic & medicinal chemistry, 16(11), 6252-6260 (2008-05-02)
Drug-induced long QT syndrome (LQTS) can cause critical cardiovascular side effects and has accounted for the withdrawal of several drugs from the market. Blockade of the potassium ion channel encoded by the human ether-a-go-go-related gene (hERG) has been identified as
Motoi Tobita et al.
Bioorganic & medicinal chemistry letters, 15(11), 2886-2890 (2005-05-25)
HERG attracts attention as a risk factor for arrhythmia, which might trigger torsade de pointes. A highly accurate classifier of chemical compounds for inhibition of the HERG potassium channel is constructed using support vector machine. For two test sets, our
R Scott Obach et al.
Drug metabolism and disposition: the biological fate of chemicals, 36(7), 1385-1405 (2008-04-23)
We present herein a compilation and trend analysis of human i.v. pharmacokinetic data on 670 drugs representing, to our knowledge, the largest publicly available set of human clinical pharmacokinetic data. This data set provides the drug metabolism scientist with a
Radha K Shandil et al.
Antimicrobial agents and chemotherapy, 51(2), 576-582 (2006-12-06)
Members of the fluoroquinolone class are being actively evaluated for inclusion in tuberculosis chemotherapy regimens, and we sought to determine the best in vitro and pharmacodynamic predictors of in vivo efficacy in mice. MICs for Mycobacterium tuberculosis H37Rv were 0.1
Joëlle Azéma et al.
Bioorganic & medicinal chemistry, 17(15), 5396-5407 (2009-07-15)
Ciprofloxacin (CP), an antibiotic has been shown to have antiproliferative and apoptotic activities in several cancer cell lines. Moreover, several reports have highlighted the interest of increasing the lipophilicity to improve the antitumor efficacy. These studies have led us to
Stéphanie Arsène et al.
Antimicrobial agents and chemotherapy, 51(9), 3254-3258 (2007-07-11)
Fluoroquinolones are poorly active against enterococci. Recently, plasmid-borne resistance to fluoroquinolones due to the qnr gene was reported in members of the Enterobacteriaceae family. The gene encodes a pentapeptide repeat protein that protects DNA gyrase from inhibition by fluoroquinolones. We
Chengxin Zhi et al.
Journal of medicinal chemistry, 49(4), 1455-1465 (2006-02-17)
Novel Gram-positive (Gram+) antibacterial compounds consisting of a DNA polymerase IIIC (pol IIIC) inhibitor covalently connected to a topoisomerase/gyrase inhibitor are described. Specifically, 3-substituted 6-(3-ethyl-4-methylanilino)uracils (EMAUs) in which the 3-substituent is a fluoroquinolone moiety (FQ) connected by various linkers were
Kin Y Tam et al.
Journal of medicinal chemistry, 53(1), 392-401 (2009-12-02)
The permeability characteristics of 33 amphoteric drugs (about 64% zwitterions at physiological pH) were studied using the parallel artificial membrane permeability assay (PAMPA) at pH 6.5. The PAMPA data were modified to include the paracellular permeability component found in cellular
Qiang Xue et al.
Environmental science and pollution research international, 22(21), 16857-16867 (2015-06-25)
An optimized solid-phase extraction (SPE) and ultra-high performance liquid chromatography-electrospray tandem mass spectrometry (UPLC-MS/MS) method was developed for the effective analysis of 35 antibiotics including sulfonamides (SAs), quinolones (QLs), tetracyclines (TCs), macrolides (MALs), lincomycin (LIN), and chloramphenicol (CAP). The addition
Artur Beberok et al.
Pharmacological reports : PR, 67(1), 38-43 (2015-01-07)
Fluoroquinolones are a group of broad spectrum bactericidal antibiotics used to treat various infections of urinary and respiratory systems, as well as in ophthalmology and dermatology. This class of antibiotics causes toxic effects directed to pigmented tissues, what introduces a
Shigeru Izawa et al.
Journal of infection and chemotherapy : official journal of the Japan Society of Chemotherapy, 21(4), 290-295 (2015-02-03)
The purpose of this study was to evaluate which of blood or urine has the greater effect on bladder tissue concentrations of fluoroquinolones important for the treatment of urinary tract infections by measuring concentrations of fluoroquinolones in the vesical tissue
Kuntal Manna et al.
Bioorganic & medicinal chemistry letters, 19(10), 2688-2692 (2009-04-28)
2-[1-(5,8-Dihydro quinoxalino[2,3-b]indoloacetyl)-3-(1-benzofuran-2-yl)-4,5-dihydro-1H-pyrazol-5-yl] phenyl derivatives were synthesized from 2-(5,8-dihydro quinoxalino[2,3-b]indol-5-yl) acetohydrazide and (2E)-1-(1-benzofuran-2-yl)-4-phenylbut-2-en-1-ones derivatives using microwave-assisted route. The structures of all the compounds have been established on the basis of analytical and spectral data. Among the 14 compounds IPB-1, IPB-5, IPB-10
John J M Wiener et al.
Bioorganic & medicinal chemistry letters, 17(10), 2718-2722 (2007-03-27)
We have previously reported a novel class of tetrahydroindazoles that display potency against a variety of Gram-positive and Gram-negative bacteria, potentially via interaction with type II bacterial topoisomerases. Herein are reported SAR investigations of this new series. Several compounds possessing
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