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The ring-opening reactions of 1-azabicyclo[1.1.0]butane 3 with thiols 6a-f gave 3-sulfenylazetidine derivatives 7a-f in 50-92% yields. Treatment of 3 with aromatic amines 11a-e and dibenzylamine 11f in the presence of Mg(ClO(4))(2) afforded the corresponding 3-aminoazetidine derivatives 12a-f in 24-53% yields. These azetidine derivatives were introduced into the C7 position of a quinolone nucleus 8 to afford the corresponding fluoroquinolones 9a-f and 13a-f in 21-83% yields. Some of them exhibited superior antibacterial activity against quinolone-susceptible MRSA in comparison with clinically used fluoroquinolones, such as levofloxacin, ciprofloxacin, and gatifloxacin.
In this study, except for the Streptococcus species, ciprofloxacin was effective against the species responsible for severe bacterial keratitis.
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A total of 156 patients were recruited from July 2011 to June 2013 at Beijing Hospital and randomized into one of the following 10-day treatment regimens: (1) Esomeprazole 20 mg twice daily, furazolidone 100 mg twice daily, amoxicillin 1000 mg twice daily, bismuth salts 150 mg thrice daily for 10 days. (2) Esomeprazole 20 mg twice daily, levofloxacin 500 mg daily, amoxicillin 1000 mg twice daily, bismuth salts 150 mg thrice daily for 10 days. H.pylori status was re-assessed with the (13)C-urea breath test at 4 weeks after the end of therapy.
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Colistin, C/S, and minocycline were active in 50 (90.9%), 50, and 44 (80.0%) isolates, respectively, and all the other drugs were active in less than 20% of isolates. Minocycline-imipenem, minocycline-C/S, minocycline-amikacin, imipenem-tobramycin, C/S-amikacin, and C/S-tobramycin combinations showed synergistic inhibitory or bactericidal activity by TKS when the same combinations were synergistic in DDS; however, C/S-imipenem was found synergistic on DDS, but not by TKS.
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We analyzed Streptococcus pneumoniae isolates in Gifu prefecture between November 2004 and December 2004. We analyzed isolates of 160 strains from 8 medical facilities to determine antibiotic susceptibility, genotype of penicillin-binding protein (PBP) genes and macrolide resistant genes, and the serotypes of penicillin-resistant S. pneumoniae (PRSP). When referred to the classification in CLSI (formerly NCCLS), the overall incidence of penicillin-susceptible (PSSP), penicillin-intermediate (PISP) and penicillin-resistant (PRSP) were 48 (30.0%), 81 (50.6%) and 31 (19.4%) strains, respectively, and the susceptibility distribution to benzylpenicillin showed triplet peaks. The incidence of PISP and PRSP was higher in the material of throat and nasal cavity, and area of Chuno and Gifu district. The sum of the incidence of PISP and PRSP was slightly higher in inpatient-derived stains than outpatient-derived strains. The incidence that didn't possess mutations in PBP genes and macrolide-resistant genes was 6 (3.75%) and the others 154 strain (96.25%) had abnormal PBP genes or macrolide-resistant genes. The 90% of pneumococcal serotypes of PRSP 31 strains were serotype 6 (14 strains, 45.2%), 19 (7 strains, 22.6%) and 23 (7 strains, 22.6%). The MIC90 of each antibiotics was as follows; 0.1 microg/mL for panipenem, 0.2 microg/mL for imipenem and tosufloxacin, 0.39 microg/mL for meropenem and gatifloxacin, 0.78 microg/mL for amoxicillin, cefteram and cefditoren, 1.56 microg/mL for piperacillin, cefcapene and levofloxacin, 3.13 microg/mL for flomoxef, 6.25 microg/mL for cefdinir and cefotiam, 12.5 microg/mL for norfloxacin and minocycline, 25 microg/mL for cefixime, and 100 microg/mL for clarithromycin.
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Regimens tested are competitive with other PPI-based treatments. One-week triple therapy containing rabeprazole plus, levofloxacin, and high-dose clarithromycin yielded a higher eradicating rate than the one containing low-dose clarithromycin and may be considered as a first-line therapy option.
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The incidence of tuberculosis is slightly higher among heart transplantation cases than in the general population in Taiwan. Tuberculosis shows a high mortality rate ranging from 22% to 31% in transplant recipients. From October 1987 to October 2007, we performed 315 heart transplantations. Clinical records were reviewed for demographic data, clinical presentation, treatment, and outcome. Tuberculosis was diagnosed by cultures of any body sample in association with compatible symptoms and signs. Mortality was related to tuberculosis if there was evidence of active tuberculosis at the time of death and no other etiology accounted for death. Ten patients who had received heart transplants were diagnosed as tuberculosis. There were seven pulmonary lesions and seven extrapulmonary lesions. Treatment consisted of isoniazid, rifampin, ethambutol, pyrazinamide, streptomycin, ciprofloxacin, and levofloxacin. Seven patients completed the antituberculosis treatment: the median treatment duration was 1 year. Three patients developed hepatitis. There was no tuberculosis-related mortality. Ten out of a total of 315 patients (3.17%) represented a tuberculosis rate higher than that reported for the general Taiwan population (67/100,000). This high mortality of infection may be completely treated by a combination of at least three drugs except pyrzinamide because of side effects and tolerance.
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A 19-year-old male patient developed ofloxacin/levofloxacin-induced rhabdomyolysis during admission for periorbital cellulitis. Symptoms of myalgia, weakness, and swelling of the arms developed after 3 days of treatment with ofloxacin 800 mg/day. Laboratory analysis confirmed the presence of urine myoglobin (381.2 microg/L) and a marked increase in serum myoglobin (590.8 microg/L), along with marked elevations in serum creatine kinase (up to 16 546 IU/L).