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Selective small-molecule inhibition of an RNA structural element
The discovery and characterization of ribocil is reported, a highly selective chemical modulator of bacterial riboflavin riboswitches that acts as a structurally distinct synthetic mimic of the natural ligand, flavin mononucleotide, to repress riboswitch-mediated ribB gene expression and inhibit bacterial cell growth.
Perinerin, a novel antimicrobial peptide purified from the clamworm Perinereis aibuhitensis grube and its partial characterization.
Results suggest that Perinerin has the potential to serve as a convenient "evaluation marker" for studying alterations in the biochemistry of the host, particularly with respect to environmental changes and the MTS-PMS colorimetric assay examination of antimicrobial activity appears to be superior to existing methods and may offer more general application in the search for new antibiotics.
Discovery of (1R,5S)-N-[3-amino-1-(cyclobutylmethyl)-2,3-dioxopropyl]- 3-[2(S)-[[[(1,1-dimethylethyl)amino]carbonyl]amino]-3,3-dimethyl-1-oxobutyl]-…
- S. Venkatraman, S. Bogen, F. G. Njoroge
- Biology, ChemistryJournal of medicinal chemistry
- 7 September 2006
The SAR leading to the discovery of 70 (SCH 503034), a novel, potent, selective, orally bioavailable NS3 protease inhibitor that has been advanced to clinical trials in human beings for the treatment of hepatitis C viral infections is described.
Second-generation highly potent and selective inhibitors of the hepatitis C virus NS3 serine protease.
- Kevin X. Chen, L. Nair, F. G. Njoroge
- Chemistry, BiologyJournal of medicinal chemistry
- 5 February 2009
Systematic optimization of different positions (P', P3, and P1) of the inhibitor resulted in the identification of the lead compound 46, which had an excellent potency and good pharmacokinetic profile and good bioavailability in rats and dogs, respectively.
Aminoglycoside complexation with a DNA.RNA hybrid duplex: the thermodynamics of recognition and inhibition of RNA processing enzymes.
- C. M. Barbieri, Tsai-Kun Li, D. S. Pilch
- Biology, ChemistryJournal of the American Chemical Society
- 2 May 2003
RNA hybrid duplex inhibits both RNase H- and RNase A-mediated cleavage of the RNA strand in the DNA and induces CD changes consistent with a shift from an A-like to a more canonical A-conformation.
Synthesis of Unprecedented Sulfonylated Phosphono-exo-Glycals Designed as Inhibitors of the Three Mycobacterial Galactofuranose Processing Enzymes.
A new methodology to synthesize exo-glycals bearing both a sulfone and a phosphonate and was applied to eight different carbohydrates from the furanose and pyranose series, finding that the Z/E configurations of these tetrasubstituted enol ethers could be ascertained using NMR spectroscopic techniques.
The introduction of P4 substituted 1-methylcyclohexyl groups into Boceprevir: a change in direction in the search for a second generation HCV NS3 protease inhibitor.
Identification of inhibitors targeting Mycobacterium tuberculosis cell wall biosynthesis via dynamic combinatorial chemistry.
A dynamic combinatorial approach along with highly efficient in situ screening to identify inhibitors of UDP-galactopyranose mutase (UGM), an essential enzyme involved in mycobacterial cell wall biosynthesis, leading to the identification of a new UGM inhibitor chemotype.
Hepatitis C virus NS3-4A serine protease inhibitors: SAR of new P1 derivatives of SCH 503034.
Concise syntheses of bacteriohopanetetrol and its glucosamine derivative.
- W. Pan, Yongming Zhang, Guang-yi Liang, S. Vincent, P. Sinaÿ
- ChemistryChemical communications
- 1 July 2005
This study describes the syntheses of bacteriohopanetetrol and its glucosamine derivative through a key direct coupling of a ribose derivative to the hopane skeleton.