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Volumn 16, Issue 18, 2008, Pages 8587-8591

Synthesis, biological evaluation and SAR study of novel pyrazole analogues as inhibitors of Mycobacterium tuberculosis

Author keywords

5 Hydroxy pyrazole; Pyrazolone; SAR study; Tuberculosis

Indexed keywords

5 HYDROXY PYRAZOLE DERIVATIVE; ANTIMYCOBACTERIAL AGENT; PYRAZOLE DERIVATIVE; PYRAZOLONE DERIVATIVE; UNCLASSIFIED DRUG;

EID: 51449117872     PISSN: 09680896     EISSN: None     Source Type: Journal    
DOI: 10.1016/j.bmc.2008.08.016     Document Type: Article
Times cited : (135)

References (24)
  • 1
    • 51449098838 scopus 로고    scopus 로고
    • World Health Organization: The World Health Organization Global Tuberculosis Program, 2007. http://www.who.int/gtb/.http://www.who.int/tb/publications/global_report/2007/pdf/full.
    • World Health Organization: The World Health Organization Global Tuberculosis Program, 2007. http://www.who.int/gtb/.http://www.who.int/tb/publications/global_report/2007/pdf/full.
  • 5
    • 51449102351 scopus 로고    scopus 로고
    • World Health Organization, TB Home, 2007. http://www.who.int/tb/en/.
    • World Health Organization, TB Home, 2007. http://www.who.int/tb/en/.
  • 11
    • 51449114915 scopus 로고    scopus 로고
    • 1H NMR analysis revealed the presence of a single signal set due to the quick chemical exchange between the three tautomeric forms.
    • 1H NMR analysis revealed the presence of a single signal set due to the quick chemical exchange between the three tautomeric forms.
  • 16
    • 51449096452 scopus 로고    scopus 로고
    • NOE interactions between benzyl protons and methyl at C3 was revealed, whereas no NOE interactions between benzyl and p-chlorophenyl protons were observed.
    • NOE interactions between benzyl protons and methyl at C3 was revealed, whereas no NOE interactions between benzyl and p-chlorophenyl protons were observed.
  • 17
    • 51449100812 scopus 로고    scopus 로고
    • Catalyst, version 4.10, Accelrys Inc., San Diego, CA. http://www.accelrys.com.
    • Catalyst, version 4.10, Accelrys Inc., San Diego, CA. http://www.accelrys.com.
  • 19
    • 51449109611 scopus 로고    scopus 로고
    • The weaker activity of fluoro-derivative 3 seems to be in contrast with pharmacophoric investigations and biological data of the other N1-p-halogen compounds. However, we hypothesised that the electron-withdrawing fluorine atom might have an inductive effect on the pyrazole nucleus and alteration of its electronic nature might resolve into a loss of activity.
    • The weaker activity of fluoro-derivative 3 seems to be in contrast with pharmacophoric investigations and biological data of the other N1-p-halogen compounds. However, we hypothesised that the electron-withdrawing fluorine atom might have an inductive effect on the pyrazole nucleus and alteration of its electronic nature might resolve into a loss of activity.


* 이 정보는 Elsevier사의 SCOPUS DB에서 KISTI가 분석하여 추출한 것입니다.