메뉴 건너뛰기
Angewandte Chemie - International Edition
Volumn 47, Issue 15, 2008, Pages 2808-2812
Anti-MRSA agent discovery using diversity-oriented synthesis
Author keywords

Antibiotics; Combinatorial chemistry; Diversity oriented synthesis; Synthesis design
Indexed keywords

CHEMICAL REACTIONS;
EID: 42249095476     PISSN: 14337851     EISSN: None     Source Type: Journal    
DOI: 10.1002/anie.200705415     Document Type: Article
Times cited : (121)
References (43)
  • 4
    • 33746001269 scopus 로고    scopus 로고
    • Angew. Chem. Int. Ed. 2006, 45, 5072-5129.
    • (2006) Angew. Chem. Int. Ed , vol.45 , pp. 5072-5129
  • 8
    • 4544291065 scopus 로고    scopus 로고
    • Angew. Chem. Int. Ed. 2004, 43, 2574-2576.
    • (2004) Angew. Chem. Int. Ed , vol.43 , pp. 2574-2576
  • 10
    • 53549129651 scopus 로고    scopus 로고
    • It is important to note that the structural diversity of natural antibiotics arises from a directed evolutionary process. Diversity-oriented synthesis lacks an evolutionary fitness check in this sense, but this shortcoming can be counteracted by successive iterations of screening and synthesis and by the intuition of experienced medicinal chemists. Another way to add an element of evolutionary advantage is to base a DOS on so-called privileged' structures, that is, those structural motifs common to bioactive molecules. The rationale behind this approach is that compounds that structurally resemble natural products are more likely to exhibit bioactivity. For an excellent discussion of this issue, see: R. Breinbauer, I. R. Vetter, H. Waldmann, Angew. Chem. 2002, 114, 3002-3015;
    • It is important to note that the structural diversity of natural antibiotics arises from a directed evolutionary process. Diversity-oriented synthesis lacks an evolutionary fitness check in this sense, but this shortcoming can be counteracted by successive iterations of screening and synthesis and by the intuition of experienced medicinal chemists. Another way to add an element of evolutionary advantage is to base a DOS on so-called "privileged' structures, that is, those structural motifs common to bioactive molecules. The rationale behind this approach is that compounds that structurally resemble natural products are more likely to exhibit bioactivity. For an excellent discussion of this issue, see: R. Breinbauer, I. R. Vetter, H. Waldmann, Angew. Chem. 2002, 114, 3002-3015;
  • 11
    • 0037119336 scopus 로고    scopus 로고
    • Angew. Chem. Int. Ed. 2002, 41, 2878-2890.
    • (2002) Angew. Chem. Int. Ed , vol.41 , pp. 2878-2890
  • 12
  • 15
  • 19
  • 24
    • 33746272686 scopus 로고    scopus 로고
    • Angew. Chem. Int. Ed. 2006, 45, 3635-3638.
    • (2006) Angew. Chem. Int. Ed , vol.45 , pp. 3635-3638
  • 26
    • 33744475697 scopus 로고    scopus 로고
    • Angew. Chem. Int. Ed. 2006, 45, 1722-1726.
    • (2006) Angew. Chem. Int. Ed , vol.45 , pp. 1722-1726
  • 38
    • 53549100620 scopus 로고    scopus 로고
    • Elsevier MDL
    • MDL Drug Data Report, Elsevier MDL, http://www.mdli.com.
    • MDL Drug Data Report
  • 39
    • 53549111773 scopus 로고    scopus 로고
    • Using this descriptor space, antibacterials cluster in a certain area of chemical space, but to a relatively small extent compared to the whole MDDR space. The clustering is also visible from the table in Figure 1 showing that antibacterials occupy less of chemical space per compound than the set of all drugs
    • Using this descriptor space, antibacterials cluster in a certain area of chemical space, but to a relatively small extent compared to the whole MDDR space. The clustering is also visible from the table in Figure 1 showing that antibacterials occupy less volume of chemical space per compound than the set of all drugs.
  • 42
    • 0034916443 scopus 로고    scopus 로고
    • A. P. Johnson, H. M. Aucken, S. Cavendish, M. Ganner, M. C. J. Wale, M. Warner, D. M. Livermore, B. D. Cookson, the UK EARSS participants, J. Antimicrob. Chemother. 2001, 48, 143-144.
    • A. P. Johnson, H. M. Aucken, S. Cavendish, M. Ganner, M. C. J. Wale, M. Warner, D. M. Livermore, B. D. Cookson, the UK EARSS participants, J. Antimicrob. Chemother. 2001, 48, 143-144.

* 이 정보는 Elsevier사의 SCOPUS DB에서 KISTI가 분석하여 추출한 것입니다.