The application of multi-component reactions in drug discovery

被引:534
作者
Weber, L [1 ]
机构
[1] Morphochem AG, D-81379 Munich, Germany
关键词
multi-component reactions; MCR; chemical diversity; diversity oriented synthesis; drug discovery; chemical libraries; lead finding; lead optimisation;
D O I
10.2174/0929867023368719
中图分类号
Q5 [生物化学]; Q7 [分子生物学];
学科分类号
071010 ; 081704 ;
摘要
Multi-component reactions (MCRs) enable the facile, automated and high throughput generation of small organic molecules. MCRs have been used to create diversity oriented and biased combinatorial libraries, to accomplish the synthesis of highly complex natural products as well as for the large-scale production of drug candidates. This provides medicinal chemists with a powerful tool to create novel chemical diversity, matching the space of biological targets with relevant chemistry. The discovery of novel MCRs has become an increasingly active area of research, yielding novel chemical scaffolds for drug discovery efforts.
引用
收藏
页码:2085 / 2093
页数:9
相关论文
共 29 条
  • [1] Pyrimidinylimidazole inhibitors of p38: Cyclic N-1 imidazole substituents enhance p38 kinase inhibition and oral activity
    Adams, JL
    Boehm, JC
    Gallagher, TF
    Kassis, S
    Webb, EF
    Hall, R
    Sorenson, M
    Garigipati, R
    Griswold, DE
    Lee, JC
    [J]. BIOORGANIC & MEDICINAL CHEMISTRY LETTERS, 2001, 11 (21) : 2867 - 2870
  • [2] Passerini multicomponent reaction of protected α-aminoaldehydes as a tool for combinatorial synthesis of enzyme inhibitors
    Banfi, L
    Guanti, G
    Riva, R
    [J]. CHEMICAL COMMUNICATIONS, 2000, (11) : 985 - 986
  • [3] A novel three-component butenolide synthesis
    Beck, B
    Magnin-Lachaux, M
    Herdtweck, E
    Dömling, A
    [J]. ORGANIC LETTERS, 2001, 3 (18) : 2875 - 2878
  • [4] CAPPI MW, 2000, Patent No. 10041402
  • [5] Enantioselective total synthesis of ecteinascidin 743
    Corey, EJ
    Gin, DY
    Kania, RS
    [J]. JOURNAL OF THE AMERICAN CHEMICAL SOCIETY, 1996, 118 (38) : 9202 - 9203
  • [6] THE 7-COMPONENT REACTION
    DOMLING, A
    UGI, I
    [J]. ANGEWANDTE CHEMIE-INTERNATIONAL EDITION IN ENGLISH, 1993, 32 (04): : 563 - 564
  • [7] Recent advances in isocyanide-based multicomponent chemistry
    Dömling, A
    [J]. CURRENT OPINION IN CHEMICAL BIOLOGY, 2002, 6 (03) : 306 - 313
  • [8] Total synthesis of ecteinascidin 743
    Endo, A
    Yanagisawa, A
    Abe, M
    Tohma, S
    Kan, T
    Fukuyama, T
    [J]. JOURNAL OF THE AMERICAN CHEMICAL SOCIETY, 2002, 124 (23) : 6552 - 6554
  • [9] Floyd CD, 1998, SYNLETT, P637
  • [10] GROBKE K, 1999, Patent No. 0921116