Published in J Med Chem on May 09, 2002
Challenges of antibacterial discovery. Clin Microbiol Rev (2011) 3.94
Prospects for aminoacyl-tRNA synthetase inhibitors as new antimicrobial agents. Antimicrob Agents Chemother (2005) 1.71
Brucella melitensis Methionyl-tRNA-Synthetase (MetRS), a Potential Drug Target for Brucellosis. PLoS One (2016) 1.39
Selective inhibitors of methionyl-tRNA synthetase have potent activity against Trypanosoma brucei Infection in Mice. Antimicrob Agents Chemother (2011) 1.37
Urea-based inhibitors of Trypanosoma brucei methionyl-tRNA synthetase: selectivity and in vivo characterization. J Med Chem (2012) 1.35
Identification of new drug targets and resistance mechanisms in Mycobacterium tuberculosis. PLoS One (2013) 1.31
Mode of action and biochemical characterization of REP8839, a novel inhibitor of methionyl-tRNA synthetase. Antimicrob Agents Chemother (2005) 1.26
Variable sensitivity to bacterial methionyl-tRNA synthetase inhibitors reveals subpopulations of Streptococcus pneumoniae with two distinct methionyl-tRNA synthetase genes. Antimicrob Agents Chemother (2003) 1.21
Horizontal transfer of drug-resistant aminoacyl-transfer-RNA synthetases of anthrax and Gram-positive pathogens. EMBO Rep (2003) 1.20
Distinct states of methionyl-tRNA synthetase indicate inhibitor binding by conformational selection. Structure (2012) 1.18
Antibacterial activity of REP8839, a new antibiotic for topical use. Antimicrob Agents Chemother (2005) 1.09
Inhibition of methionyl-tRNA synthetase by REP8839 and effects of resistance mutations on enzyme activity. Antimicrob Agents Chemother (2008) 1.01
N-O chemistry for antibiotics: discovery of N-alkyl-N-(pyridin-2-yl)hydroxylamine scaffolds as selective antibacterial agents using nitroso Diels-Alder and ene chemistry. J Med Chem (2011) 0.96
Structure of Leishmania major methionyl-tRNA synthetase in complex with intermediate products methionyladenylate and pyrophosphate. Biochimie (2010) 0.93
Inhibitors of Methionyl-tRNA Synthetase Have Potent Activity against Giardia intestinalis Trophozoites. Antimicrob Agents Chemother (2015) 0.87
5-Fluoroimidazo[4,5-b]pyridine Is a Privileged Fragment That Conveys Bioavailability to Potent Trypanosomal Methionyl-tRNA Synthetase Inhibitors. ACS Infect Dis (2016) 0.83
Structure-guided design of novel Trypanosoma brucei Methionyl-tRNA synthetase inhibitors. Eur J Med Chem (2016) 0.80
Inhibition of protein synthesis and malaria parasite development by drug targeting of methionyl-tRNA synthetases. Antimicrob Agents Chemother (2015) 0.79
Novel hybrid virtual screening protocol based on molecular docking and structure-based pharmacophore for discovery of methionyl-tRNA synthetase inhibitors as antibacterial agents. Int J Mol Sci (2013) 0.78
Essentiality Assessment of Cysteinyl and Lysyl-tRNA Synthetases of Mycobacterium smegmatis. PLoS One (2016) 0.76
Crystallization of Mycobacterium smegmatis methionyl-tRNA synthetase in the presence of methionine and adenosine. Acta Crystallogr Sect F Struct Biol Cryst Commun (2009) 0.76
A homology model for Clostridium difficile methionyl tRNA synthetase: active site analysis and docking interactions. J Mol Model (2010) 0.75
Synthesis and fungicidal activity of pyrazole derivatives containing 1,2,3,4-tetrahydroquinoline. Chem Cent J (2016) 0.75
Development of methionyl-tRNA synthetase inhibitors as antibiotics for Gram-positive bacterial infections. Antimicrob Agents Chemother (2017) 0.75
Optimization of a binding fragment targeting the "enlarged methionine pocket" leads to potent Trypanosoma brucei methionyl-tRNA synthetase inhibitors. Bioorg Med Chem Lett (2017) 0.75
A selective jumonji H3K27 demethylase inhibitor modulates the proinflammatory macrophage response. Nature (2012) 4.08
Type IIA topoisomerase inhibition by a new class of antibacterial agents. Nature (2010) 3.58
Discovery of a novel and potent class of FabI-directed antibacterial agents. Antimicrob Agents Chemother (2002) 2.14
Structural basis of quinolone inhibition of type IIA topoisomerases and target-mediated resistance. Nat Struct Mol Biol (2010) 1.45
Discovery of aminopyridine-based inhibitors of bacterial enoyl-ACP reductase (FabI). J Med Chem (2002) 1.44
A standard operating procedure for assessing liquid handler performance in high-throughput screening. J Biomol Screen (2002) 1.34
Development and validation of reagents and assays for EZH2 peptide and nucleosome high-throughput screens. J Biomol Screen (2012) 1.30
GSK189254, a novel H3 receptor antagonist that binds to histamine H3 receptors in Alzheimer's disease brain and improves cognitive performance in preclinical models. J Pharmacol Exp Ther (2007) 1.30
Variable sensitivity to bacterial methionyl-tRNA synthetase inhibitors reveals subpopulations of Streptococcus pneumoniae with two distinct methionyl-tRNA synthetase genes. Antimicrob Agents Chemother (2003) 1.21
Selectivity of kinase inhibitor fragments. J Med Chem (2011) 1.05
Nuclear magnetic resonance spectroscopy reveals the functional state of the signalling protein CheY in vivo in Escherichia coli. Mol Microbiol (2003) 1.05
Definition of the heterocyclic pharmacophore of bacterial methionyl tRNA synthetase inhibitors: potent antibacterially active non-quinolone analogues. Bioorg Med Chem Lett (2004) 1.05
1,2,4-triazol-3-yl-thiopropyl-tetrahydrobenzazepines: a series of potent and selective dopamine D(3) receptor antagonists. J Med Chem (2007) 1.02
N-(3-Cyano-4,5,6,7-tetrahydro-1-benzothien-2-yl)amides as potent, selective, inhibitors of JNK2 and JNK3. Bioorg Med Chem Lett (2006) 0.99
Perspectives on the discovery of small-molecule modulators for epigenetic processes. J Biomol Screen (2012) 0.94
Discovery and optimisation of potent, selective, ethanolamine inhibitors of bacterial phenylalanyl tRNA synthetase. Bioorg Med Chem Lett (2005) 0.94
1,2,4-Triazolyl azabicyclo[3.1.0]hexanes: a new series of potent and selective dopamine D(3) receptor antagonists. J Med Chem (2010) 0.92
Optimisation of aryl substitution leading to potent methionyl tRNA synthetase inhibitors with excellent gram-positive antibacterial activity. Bioorg Med Chem Lett (2003) 0.91
Identification of a series of tricyclic natural products as potent broad-spectrum inhibitors of metallo-beta-lactamases. Antimicrob Agents Chemother (2002) 0.91
The antimicrobial natural product chuangxinmycin and some synthetic analogues are potent and selective inhibitors of bacterial tryptophanyl tRNA synthetase. Bioorg Med Chem Lett (2002) 0.88
Fragment-Based Discovery of Low-Micromolar ATAD2 Bromodomain Inhibitors. J Med Chem (2015) 0.87
Concise synthesis, preparative resolution, absolute configuration determination, and applications of an atropisomeric biaryl catalyst for asymmetric acylation. J Org Chem (2003) 0.87
Novel amino-piperidines as potent antibacterials targeting bacterial type IIA topoisomerases. Bioorg Med Chem Lett (2011) 0.87
Synthesis and biological evaluations of P4-benzoxaborole-substituted macrocyclic inhibitors of HCV NS3 protease. Bioorg Med Chem Lett (2010) 0.85
Synthesis and pharmacological characterization of novel druglike corticotropin-releasing factor 1 antagonists. J Med Chem (2008) 0.85
Single-molecule detection technologies in miniaturized high-throughput screening: fluorescence intensity distribution analysis. J Biomol Screen (2003) 0.84
Novel cyclohexyl-amides as potent antibacterials targeting bacterial type IIA topoisomerases. Bioorg Med Chem Lett (2011) 0.84
Development of a 1-microl scale assay for mitogen-activated kinase kinase 7 using 2-D fluorescence intensity distribution analysis anisotropy. J Biomol Screen (2002) 0.83
Exploration of the amine terminus in a novel series of 1,2,4-triazolo-3-yl-azabicyclo[3.1.0]hexanes as selective dopamine D3 receptor antagonists. J Med Chem (2010) 0.83
Optimization of novel acyl pyrrolidine inhibitors of hepatitis C virus RNA-dependent RNA polymerase leading to a development candidate. J Med Chem (2007) 0.83
Structure-Based Optimization of Naphthyridones into Potent ATAD2 Bromodomain Inhibitors. J Med Chem (2015) 0.83
Potential of real-time measurement of GFP-fusion proteins. J Biotechnol (2004) 0.83
Confirmation of the antibacterial mode of action of SB-219383, a novel tyrosyl tRNA synthetase inhibitor from a Micromonospora sp. J Antibiot (Tokyo) (2002) 0.82
Synthesis and evaluation of novel alpha-amino cyclic boronates as inhibitors of HCV NS3 protease. Bioorg Med Chem Lett (2010) 0.81
Studies towards the identification of a new generation of atypical antipsychotic agents. Bioorg Med Chem Lett (2006) 0.81
High-yield production and characterization of biologically active GST-tagged human topoisomerase IIα protein in insect cells for the development of a high-throughput assay. Protein Expr Purif (2010) 0.81
A novel approach applying a chemical biology strategy in phenotypic screening reveals pathway-selective regulators of histone 3 K27 tri-methylation. Mol Biosyst (2014) 0.80
Conformational restriction of methionyl tRNA synthetase inhibitors leading to analogues with potent inhibition and excellent gram-positive antibacterial activity. Bioorg Med Chem Lett (2003) 0.80
Synthesis and SAR of acyclic HCV NS3 protease inhibitors with novel P4-benzoxaborole moieties. Bioorg Med Chem Lett (2011) 0.80
The effect of antibiotic treatment on the intracellular nucleotide pools of Staphylococcus aureus. FEMS Microbiol Lett (2002) 0.79
New fused benzazepine as selective D3 receptor antagonists. Synthesis and biological evaluation. Part one: [h]-fused tricyclic systems. Bioorg Med Chem Lett (2008) 0.79
Discovery and biochemical characterization of Plasmodium thioredoxin reductase inhibitors from an antimalarial set. Biochemistry (2012) 0.79
Pharmacological profile of antipsychotics at monoamine receptors: atypicality beyond 5-HT2A receptor blockade. CNS Neurol Disord Drug Targets (2006) 0.78
Synthesis of new acylsulfamoyl benzoxaboroles as potent inhibitors of HCV NS3 protease. Bioorg Med Chem Lett (2010) 0.78
New fused benzazepine as selective D3 receptor antagonists. Synthesis and biological evaluation. Part 2: [g]-fused and hetero-fused systems. Bioorg Med Chem Lett (2008) 0.78
Identification of clinical candidates from the benzazepine class of histamine H3 receptor antagonists. Bioorg Med Chem Lett (2013) 0.78
Novel substituted tetrahydrotriazaacenaphthylene derivatives as potent CRF1 receptor antagonists. Bioorg Med Chem Lett (2007) 0.78
Development of phenotypic screening assays for γ-globin induction using primary human bone marrow day 7 erythroid progenitor cells. J Biomol Screen (2013) 0.77
Dihydropyrrole[2,3-d]pyridine derivatives as novel corticotropin-releasing factor-1 antagonists: mapping of the receptor binding pocket by in silico docking studies. J Med Chem (2008) 0.77
SAR of biphenyl carboxamide ligands of the human melanin-concentrating hormone receptor 1 (MCH R1): discovery of antagonist SB-568849. Bioorg Med Chem Lett (2006) 0.77
Triazolyl azabicyclo[3.1.0]hexanes: A class of potent and selective dopamine D(3) receptor antagonists. ChemMedChem (2010) 0.77
Synthesis and activity of analogues of the isoleucyl tRNA synthetase inhibitor SB-203207. Bioorg Med Chem (2003) 0.77
Heteroaryl-substituted 4-(1H-pyrazol-1-yl)-5,6-dihydro-1H-pyrrolo[2,3-d]pyrimidine derivatives as potent and selective corticotropin-releasing factor receptor-1 antagonists. ChemMedChem (2008) 0.76
Novel macrocyclic HCV NS3 protease inhibitors derived from α-amino cyclic boronates. Bioorg Med Chem Lett (2010) 0.76
6-Alkylquinolone-3-carboxylic acid tethered to macrolides synthesis and antimicrobial profile. Bioorg Med Chem (2010) 0.76
Discovery of novel urea-based hepatitis C protease inhibitors with high potency against protease-inhibitor-resistant mutants. J Med Chem (2012) 0.76
Synthesis and properties of macrolones characterized by two ether bonds in the linker. Bioorg Med Chem (2010) 0.76
Dopamine D3 receptor antagonists: the quest for a potentially selective PET ligand. Part one: lead identification. Bioorg Med Chem Lett (2009) 0.75
Dopamine D(3) receptor antagonists: The quest for a potentially selective PET ligand. Part two: Lead optimization. Bioorg Med Chem Lett (2009) 0.75
[2,3]-Sigmatropic rearrangement of allylic selenimides: strategy for the synthesis of peptides, peptidomimetics, and N-aryl vinyl glycines. J Org Chem (2014) 0.75
5-{2-[4-(2-methyl-5-quinolinyl)-1-piperazinyl]ethyl}-2(1H)-quinolinones and 3,4-dihydro-2(1H)-quinolinones: dual-acting 5-HT1 receptor antagonists and serotonin reuptake inhibitors. Part 3. Bioorg Med Chem Lett (2010) 0.75
Discovery of potent and stable conformationally constrained analogues of the MCH R1 antagonist SB-568849. Bioorg Med Chem Lett (2006) 0.75
Development of an insect-cell-based assay for detection of kinase inhibition using NF-kappaB-inducing kinase as a paradigm. Biochem J (2009) 0.75
1-Heteroaryl-6-(3,4-dichlorophenyl)-3-azabicyclo[4.1.0]heptane: further insights into a class of triple re-uptake inhibitors. Bioorg Med Chem (2011) 0.75
NanoStore: a concept for logistical improvements of compound handling in high-throughput screening. J Biomol Screen (2005) 0.75
The identification of a selective dopamine D2 partial agonist, D3 antagonist displaying high levels of brain exposure. Bioorg Med Chem Lett (2010) 0.75
The discovery of the benzazepine class of histamine H3 receptor antagonists. Bioorg Med Chem Lett (2013) 0.75
S-alkyl dithioformates as 1,3-dipolarophiles. Generation of C(2)-unsubstituted penems. Org Lett (2004) 0.75
Synthesis and antiviral activity of novel HCV NS3 protease inhibitors with P4 capping groups. Bioorg Med Chem Lett (2012) 0.75