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Volumn 15, Issue 11, 2005, Pages 2834-2839

Synthesis and antibacterial activity of dihydro-1,2-oxazine and 2-pyrazoline oxazolidinones: Novel analogs of linezolid

Author keywords

Antibacterial; Linezolid; Oxazolidinones

Indexed keywords

1,2 OXAZINE DERIVATIVE; ALKADIENE; EPEREZOLID; LINEZOLID; NITROSAMINE; OXAZOLIDINE DERIVATIVE; PYRAZOLINE DERIVATIVE;

EID: 19544392166     PISSN: 0960894X     EISSN: None     Source Type: Journal    
DOI: 10.1016/j.bmcl.2005.03.099     Document Type: Article
Times cited : (48)

References (26)
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    • 0038441366 scopus 로고    scopus 로고
    • Ethan Rubinstein, MD. 43rd Intersci. Conf. Antimicrob Agents Chemother (ICAAC), September 14-17, 2003, Session 176(F,L) abstract#1782. (The need for an improved hematological profile is less clear cut for routine therapy: analysis of safety assessments on 2046 Zyvox patients and 2001 comparator drug-treated patients from seven Phase III clinical trials indicated virtually no differences in effects on hemoglobin, neutrophil, or platelet counts over the first 14 days of therapy. See: E. Rubinstein, R. Isturiz, H.C. Standiford, L.G. Smith, T.H. Oliphant, S. Cammarata, B. Hafkin, V. Le, and J. Remington Antimicrob. Agents Chemother. 47 2003 1824 1831)
    • (2003) Antimicrob. Agents Chemother. , vol.47 , pp. 1824-1831
    • Rubinstein, E.1    Isturiz, R.2    Standiford, H.C.3    Smith, L.G.4    Oliphant, T.H.5    Cammarata, S.6    Hafkin, B.7    Le, V.8    Remington, J.9
  • 5
    • 19544365783 scopus 로고    scopus 로고
    • note
    • Most of the oxazolidinones reported by Upjohn/Pharmacia to have superior safety profiles in a 30-day rat toxicity model have donating nitrogens in the para-position of the phenyl group. These agents include linezolid, eperezolid, U-100480 (thiomorpholine), and U-97456 (indoline). See Ref. 1. DuPont agents DuP-721 and DuP-105 lacking a para-amine functionality had more severe toxicity in a 30-day rat model (in house data)
  • 8
    • 19544384624 scopus 로고    scopus 로고
    • PCT. WO2003027083-A1, April 03, 2003
    • Fukuda, Y.; Hammond, M. L. PCT. WO2003027083-A1, April 03, 2003
    • Fukuda, Y.1    Hammond, M.L.2
  • 9
    • 0035169586 scopus 로고    scopus 로고
    • For a discussion of 3D-QSAR of 3-aryloxazolidinone antibacterials see: R.G. Karki, and V.M. Kulkarni Bioorg. Med. Chem. 9 2001 3153 3160
    • (2001) Bioorg. Med. Chem. , vol.9 , pp. 3153-3160
    • Karki, R.G.1    Kulkarni, V.M.2
  • 19
    • 19544365135 scopus 로고    scopus 로고
    • Ihara Chem Ind Co Ltd; Japan Patent, JP-04244067, 92-337745, 1992
    • Ihara Chem Ind Co Ltd; Japan Patent, JP-04244067, 92-337745, 1992
  • 21
    • 19544370434 scopus 로고    scopus 로고
    • note
    • 2). The MIC was defined as the lowest drug concentration that prevented physical growth
  • 23
    • 19544373186 scopus 로고    scopus 로고
    • note
    • The MIC of 25 against Streptococcus pneumoniae A9585 is actually quite impressive, but this determination was not repeated. Also, compound 25 had MIC's of 8 μg/mL against two other strains (S. pneumoniae A27881 and S. pneumoniae A28272) not included in Table 1
  • 25
    • 19544379600 scopus 로고    scopus 로고
    • note
    • Staphylococcus aureus/Pen+ A15090, Inoculum 1.05 × 107 cfu/mouse ip in 7% mucin, drugs dissolved in 10% DMSO, 5% Tw-80, and water, administered orally b.i.d., 1 and 5 h post infection, death recorded for 8 days, 10 mice per group
  • 26
    • 19544376724 scopus 로고    scopus 로고
    • note
    • 1H NMR and LC/MS)


* 이 정보는 Elsevier사의 SCOPUS DB에서 KISTI가 분석하여 추출한 것입니다.