A convenient procedure for the solution phase preparation of 2-aminothiazole combinatorial libraries

被引:108
作者
Bailey, N [1 ]
Dean, AW [1 ]
Judd, DB [1 ]
Middlemiss, D [1 ]
Storer, R [1 ]
Watson, SP [1 ]
机构
[1] GLAXOWELLCOME MED RES CTR,STEVENAGE SG1 2NY,HERTS,ENGLAND
关键词
D O I
10.1016/0960-894X(96)00241-7
中图分类号
R914 [药物化学];
学科分类号
100701 ;
摘要
A convenient procedure for the solution phase preparation of 2-aminothiazole combinatorial libraries is described. The library preparation is simple, practical, and effective, generating compounds based around a known pharmacophore in high yield and purity. Furthermore, the procedure tolerates a diverse range of functionality in its substrates and is notable in allowing the preparation of compounds containing both free acids and bases without recourse to protection. Copyright (C) 1996 Elsevier Science Ltd
引用
收藏
页码:1409 / 1414
页数:6
相关论文
共 14 条
  • [1] BARRETT RW, 1994, J MED CHEM, V37, P1385
  • [2] BARRETT RW, 1994, J MED CHEM, V37, P1233
  • [3] Hantzsch A, 1887, CHEM BER, V20, P3118, DOI [10.1002/cber.188702002200, DOI 10.1002/CBER.188702002200]
  • [4] HOGAN JC, 1995, SYNTH CHEM LIB DRUG
  • [5] GENERATION AND SCREENING OF AN OLIGONUCLEOTIDE-ENCODED SYNTHETIC PEPTIDE LIBRARY
    NEEDELS, MC
    JONES, DG
    TATE, EH
    HEINKEL, GL
    KOCHERSPERGER, LM
    DOWER, WJ
    BARRETT, RW
    GALLOP, MA
    [J]. PROCEEDINGS OF THE NATIONAL ACADEMY OF SCIENCES OF THE UNITED STATES OF AMERICA, 1993, 90 (22) : 10700 - 10704
  • [6] COMPLEX SYNTHETIC CHEMICAL LIBRARIES INDEXED WITH MOLECULAR TAGS
    OHLMEYER, MHJ
    SWANSON, RN
    DILLARD, LW
    READER, JC
    ASOULINE, G
    KOBAYASHI, R
    WIGLER, M
    STILL, WC
    [J]. PROCEEDINGS OF THE NATIONAL ACADEMY OF SCIENCES OF THE UNITED STATES OF AMERICA, 1993, 90 (23) : 10922 - 10926
  • [7] PETERSON JR, 1995, EXPL MOL DIV SMALL M
  • [8] PREPARATION AND SCREENING AGAINST ACETYLCHOLINESTERASE OF A NONPEPTIDE INDEXED COMBINATORIAL LIBRARY
    PIRRUNG, MC
    CHEN, J
    [J]. JOURNAL OF THE AMERICAN CHEMICAL SOCIETY, 1995, 117 (04) : 1240 - 1245
  • [9] SYNTHESIS AND BIOLOGICAL EVALUATION OF A LIBRARY CONTAINING POTENTIALLY 1600 AMIDES ESTERS - A STRATEGY FOR RAPID COMPOUND GENERATION AND SCREENING
    SMITH, PW
    LAI, JYQ
    WHITTINGTON, AR
    COX, B
    HOUSTON, JG
    [J]. BIOORGANIC & MEDICINAL CHEMISTRY LETTERS, 1994, 4 (24) : 2821 - 2824
  • [10] INHIBITION OF NEUTROPHIL SUPEROXIDE PRODUCTION BY FANETIZOLE
    STYRT, B
    ROCKLIN, RE
    KLEMPNER, MS
    [J]. INFLAMMATION, 1985, 9 (03) : 233 - 244