New inhibitors of bacterial protein synthesis from a combinatorial library of macrocycles

Journal of Medicinal Chemistry

Volumn 45, Issue 16, 2002, Pages 3430-3439

  Jefferson, Elizabeth A ^a   Arakawa, Satoshi ^a   Blyn, Lawrence B ^a   Miyaji, Alycia ^a   Osgood, Stephen A ^a   Ranken, Raymond ^a   Risen, Lisa M ^a   Swayze, Eric E ^a  

^a ISIS PHARMACEUTICALS   (United States)

Author keywords

[No Author keywords available]

Indexed keywords

ANTIINFECTIVE AGENT; BACTERIAL PROTEIN; BACTERIUM LIPOPOLYSACCHARIDE; MACROCYCLIC COMPOUND; PROTEIN SYNTHESIS INHIBITOR; RIBOSOME RNA;

ANTIBACTERIAL ACTIVITY; ARTICLE; BACTERIAL CELL; COMBINATORIAL LIBRARY; CONTROLLED STUDY; DRUG DETERMINATION; DRUG POTENCY; DRUG SCREENING; ESCHERICHIA COLI; GENE TARGETING; IC 50; MINIMUM INHIBITORY CONCENTRATION; NONHUMAN; PROTEIN SYNTHESIS INHIBITION; RNA TRANSLATION; STEREOCHEMISTRY; STRUCTURE ACTIVITY RELATION;

ANTI-BACTERIAL AGENTS; BACTERIAL PROTEINS; COMBINATORIAL CHEMISTRY TECHNIQUES; ESCHERICHIA COLI; HETEROCYCLIC COMPOUNDS; LIPOPOLYSACCHARIDES; MUTATION; PROTEIN BIOSYNTHESIS; QUINOXALINES; RNA, BACTERIAL; RNA, RIBOSOMAL; STRUCTURE-ACTIVITY RELATIONSHIP; TRANSCRIPTION, GENETIC;

EID: 0036682411     PISSN: 00222623     EISSN: None     Source Type: Journal    
DOI: 10.1021/jm010437x     Document Type: Article

References (46)

1. Antimicrobial-drug resistance
2. RNA as a target for small molecules
3. Strategies for the design of drugs targeting RNA and RNA-protein complexes
4. Targeting RNA with small molecules
5. Targeting RNA with small-molecule drugs: Therapeutic promise and chemical challenges
6. Interaction of aminoglycoside antibiotics with RNA
7. Interaction of antibiotics with functional sites in 16S ribosomal RNA
8. Tetracyclines, molecular and clinical aspects
9. Glycylcyclines: A new generation of tetracyclines
10. In vitro activity of RU6004, a new ketolide antibiotic, against gram-positive bacteria
11. Oxazolidinone antibacterial agents: Development of the clinical candidates eperezolid and linezolid
12. The streptogramin antibiotics: Update on their mechanism of action
13. Application of residual dipolar coupling measurements to identify conformational changes in RNA induced by antibiotics
14. Paromomycin binding induces a local conformational change in the A-site of 16S rRNA
15. Antibacterial activity of macrocycles targeting structured RNA
16. Membrane permeabilization mechanisms of a cyclic antimicrobial peptide, tachyplesin I, and its linear analog
17. Kawaguchipeptin B, an antibacterial cyclic undecapeptide from the cyanobacterium microcystis aeruginosa
18. Antibiotics A21459 A and B, new inhibitors of bacterial protein synthesis, taxonomy, isolation and characterization
19. β-Amino acid facilitates macrocyclic ring closure in a combinatorial library
20. Use of in vitro protein synthesis from polymerase chain reaction-generated templates to study interaction of Escherichia coli transcription factors with core RNA polymerase and for epitope mapping of monoclonal antibodies
21. Solid phase reductive alkylation of secondary amines
22. NAr cyclizations to form cyclic peptidomimetics of β-turns
23. NAr methodology
24. Radio frequency encoded combinatorial chemistry
25. LC/MS applications in drug development
26. Design and synthesis of new aminoglycoside antibiotics containing neamine as an optimal core structure: Correlation of antibiotic activity with in vitro inhibition of translation
27. Aminoglycoside-arginine coagulates that bind TAR RNA: Synthesis, characterization, and antiviral activity
28. Ligand based technique for the discovery of drugs targeting structured RNA
29. Characterization of low-affinity complexes between RNA and small molecules using electrospray ionization mass spectrometry
30. Crystal structure of a conserved ribosomal protein-RNA complex
31. Cooperative interactions of RNA and thiostrepton antibiotic with two domains of ribosomal protein L11
32. Inhibitors of protein-RNA complexation that target the RNA: Specific recognition of human immunodeficiency virus type I TAR RNA by small organic molecules
33. Electrostatic interactions in RNA aminoglycosides binding
34. Aminoglycoside binding to the hammerhead ribozyme: A general model for the interaction of cationic antibiotics with RNA
35. Molecular mechanisms involved in the transport of antibiotics into bacteria
36. Antibiotic efflux mechanisms
37. Molecular basis of bacterial outer membrane permeability
38. Genes acrA and acrB encode a stress-induced efflux system of Escherichia coli
39. Biochemistry and regulation of a novel Escherichia coli K-12 porin protein, OmpG, which produces unusually large channels
40. Inhibition of glucosamine-6-phosphate synthase from Candida albicans by quinoxaline-2,3-diones
41. Substituted 5- and 6-quinoxalinecarboxylic acids and their tuberculostatic activity
42. Potent hydrophilic dienophiles. Synthesis and aqueous stability of several 4-aryl- and sulfonated 4-aryl-1,2,4-triazoline-3,5-diones and their immobilization on silica gel