Discovery of the first antibacterial small molecule inhibitors of MurB

被引:82
作者
Bronson, JJ [1 ]
DenBleyker, KL [1 ]
Falk, PJ [1 ]
Mate, RA [1 ]
Ho, HT [1 ]
Pucci, MJ [1 ]
Snyder, LB [1 ]
机构
[1] Bristol Myers Squibb Co, Pharmaceut Res Inst, Wallingford, CT 06492 USA
关键词
D O I
10.1016/S0960-894X(02)01076-4
中图分类号
R914 [药物化学];
学科分类号
100701 ;
摘要
A series of imidazolinone analogues was synthesized and shown to possess potent MurB inhibitory as well as good antibacterial activity. (C) 2003 Elsevier Science Ltd. All rights reserved.
引用
收藏
页码:873 / 875
页数:3
相关论文
共 26 条
[1]   4-thiazolidinones: Novel inhibitors of the bacterial enzyme MurB [J].
Andres, CJ ;
Bronson, JJ ;
D'Andrea, SV ;
Deshpande, MS ;
Falk, PJ ;
Grant-Young, KA ;
Harte, WE ;
Ho, HT ;
Misco, PF ;
Robertson, JG ;
Stock, D ;
Sun, YX ;
Walsh, AW .
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS, 2000, 10 (08) :715-717
[2]   Spectroscopic properties of Escherichia coli UDP-N-acetylenolpyruvylglucosamine reductase [J].
Axley, MJ ;
Fairman, R ;
Yanchunas, J ;
Villafranca, JJ ;
Robertson, JG .
BIOCHEMISTRY, 1997, 36 (04) :812-822
[3]   AN ENZYME-SUBSTRATE COMPLEX INVOLVED IN BACTERIAL-CELL WALL BIOSYNTHESIS [J].
BENSON, TE ;
FILMAN, DJ ;
WALSH, CT ;
HOGLE, JM .
NATURE STRUCTURAL BIOLOGY, 1995, 2 (08) :644-653
[4]   X-ray crystal structures of the S229A mutant and wild-type MurB in the presence of the substrate enolpyruvyl-UDP-N-acetylglucosamine at 1.8-angstrom resolution [J].
Benson, TE ;
Walsh, CT ;
Hogle, JM .
BIOCHEMISTRY, 1997, 36 (04) :806-811
[5]   The structure of the substrate-free form of MurB, an essential enzyme for the synthesis of bacterial cell walls [J].
Benson, TE ;
Walsh, CT ;
Hogle, JM .
STRUCTURE, 1996, 4 (01) :47-54
[6]   OVEREXPRESSION, PURIFICATION, AND MECHANISTIC STUDY OF UDP-N-ACETYLENOLPYRUVYLGLUCOSAMINE REDUCTASE [J].
BENSON, TE ;
MARQUARDT, JL ;
MARQUARDT, AC ;
ETZKORN, FA ;
WALSH, CT .
BIOCHEMISTRY, 1993, 32 (08) :2024-2030
[7]   Kinetic characterization of wild-type and S229A mutant MurB: Evidence for the role of ser 229 as a general acid [J].
Benson, TE ;
Walsh, CT ;
Massey, V .
BIOCHEMISTRY, 1997, 36 (04) :796-805
[8]   INTRACELLULAR STEPS OF BACTERIAL-CELL WALL PEPTIDOGLYCAN BIOSYNTHESIS - ENZYMOLOGY, ANTIBIOTICS, AND ANTIBIOTIC-RESISTANCE [J].
BUGG, TDH ;
WALSH, CT .
NATURAL PRODUCT REPORTS, 1992, 9 (03) :199-215
[9]   Peptide synthesis via amino acid halides [J].
Carpino, LA ;
Beyermann, M ;
Wenschuh, H ;
Bienert, M .
ACCOUNTS OF CHEMICAL RESEARCH, 1996, 29 (06) :268-274
[10]   TETRAMETHYLFLUOROFORMAMIDINIUM HEXAFLUOROPHOSPHATE - A RAPID-ACTING PEPTIDE COUPLING REAGENT FOR SOLUTION AND SOLID-PHASE PEPTIDE-SYNTHESIS [J].
CARPINO, LA ;
EL-FAHAM, A .
JOURNAL OF THE AMERICAN CHEMICAL SOCIETY, 1995, 117 (19) :5401-5402