Iclaprim, a novel diaminopyrimidine with potent activity on trimethoprim sensitive and resistant bacteria

被引：134

作者：

Schneider, P ^{[1
]}

Hawser, S ^{[1
]}

Islam, K ^{[1
]}

机构：

[1] Arpida Ltd, CH-4142 Muenchenstein, Switzerland

来源：

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 2003年 / 13卷 / 23期

关键词：

D O I：

10.1016/j.bmcl.2003.07.023

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

Iclaprim, a new selective dihydrofolate inhibitor was synthesized based on rational drug design. Iclaprim's interaction with a resistant Staphylococcus aureus dihydrofolate reductase (DHFR) is outlined in comparison to trimethoprim (TMP). This compound is active against methicillin, TMP and vancomycin resistant strains. Arpida Ltd. is developing Iclaprim for serious hospital infections from Gram-positive pathogens and respiratory tract infections. (C) 2003 Elsevier Ltd. All rights reserved.

引用

页码：4217 / 4221

页数：5

共 38 条

[1] [Anonymous], 42 INT C ANT AG CHEM
[2] BASIS OF SELECTIVITY OF ANTIBACTERIAL DIAMINOPYRIMIDINES
BACCANARI, DP
KUYPER, LF
[J]. JOURNAL OF CHEMOTHERAPY, 1993, 5 (06) : 393 - 399
[3] BAJAKSOUZIAN S, 2002, 42 INT C ANT AG CHEM
[4] A H-1-NMR STUDY OF THE INTERACTIONS AND CONFORMATIONS OF RATIONALLY DESIGNED BRODIMOPRIM ANALOGS IN COMPLEXES WITH LACTOBACILLUS-CASEI DIHYDROFOLATE-REDUCTASE
BIRDSALL, B
FEENEY, J
PASCUAL, C
ROBERTS, GCK
KOMPIS, I
THEN, RL
MULLER, K
KROEHN, A
[J]. JOURNAL OF MEDICINAL CHEMISTRY, 1984, 27 (12) : 1672 - 1676
[5] IDENTICAL GENES FOR TRIMETHOPRIM-RESISTANT DIHYDROFOLATE-REDUCTASE FROM STAPHYLOCOCCUS-AUREUS IN AUSTRALIA AND CENTRAL-EUROPE
BURDESKA, A
OTT, M
BANNWARTH, W
THEN, RL
[J]. FEBS LETTERS, 1990, 266 (1-2) : 159 - 162
[6] CANDIANI GP, 2002, 42 INT C ANT AG CHEM
[7] Structural studies on bioactive compounds.: 34.: Design, synthesis, and biological evaluation of triazenyl-substituted pyrimethamine inhibitors of Pneumocystis carinii dihydrofolate reductase
Chan, DCM
Laughton, CA
Queener, SF
Stevens, MFG
[J]. JOURNAL OF MEDICINAL CHEMISTRY, 2001, 44 (16) : 2555 - 2564
[8] PHENOTYPIC EXPRESSION IN ESCHERICHIA-COLI OF A DNA-SEQUENCE CODING FOR MOUSE DIHYDROFOLATE-REDUCTASE
CHANG, ACY
NUNBERG, JH
KAUFMAN, RJ
ERLICH, HA
SCHIMKE, RT
COHEN, SN
[J]. NATURE, 1978, 275 (5681) : 617 - 624
[9] A single amino acid substitution in Staphylococcus aureus dihydrofolate reductase determines trimethoprim resistance
Dale, GE
Broger, C
DArcy, A
Hartman, PG
DeHoogt, R
Jolidon, S
Kompis, I
Labhardt, AM
Langen, H
Locher, H
Page, MGP
Stuber, D
Then, RL
Wipf, B
Oefner, C
[J]. JOURNAL OF MOLECULAR BIOLOGY, 1997, 266 (01) : 23 - 30
[10] Pharmacophore mapping of a series of 2,4-diamino-5-deazapteridine inhibitors of Mycobacterium avium complex dihydrofolate reductase
Debnath, AK
[J]. JOURNAL OF MEDICINAL CHEMISTRY, 2002, 45 (01) : 41 - 53

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