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An asymmetric synthesis of 16-HETE, an endogenous inhibitor of neutrophil activity, was achieved in six steps from R -(−)-glycidyl benzyl ether in 28% overall yield.
A novel series of chromene-based TNF-α inhibitors is described. These chromene derivatives inhibit bacterial lipopolysaccharide (LPS) stimulated production of TNF-α from human peripheral blood mononuclear cells (PBMC). Additionally, these compounds inhibit NF-kB mediated transcription activation.
A novel acyl carrier protein synthase inhibitor, Sch 538415 ( 1 ), was isolated from an unidentified bacterial microbe. Structure elucidation of 1 was accomplished based on analysis of spectroscopic data including UV, MS and 2D-NMR spectra. Compound 1 exhibited inhibitory activity in the acyl...
Isopropyl substituted 4-thioazolyl valine side chains are highly optimized P 2 –P 3 ligands for C 2 symmetry-based HIV protease inhibitors, as exemplified by the drug ritonavir. Replacement of the side chain with the conformationally constrained hexahydrofurofuranyloxy P 2 ligand in combination...
Farnesyltransferase inhibitors (FTIs) have emerged as a novel class of anticancer agents. Analogues of the potent FTI, 4-(3-biphenyl-1-hydroxy-1-(3-methyl-3 H -imidazol-4-yl)-prop-2-ynyl)-1-yl-benzonitrile, were synthesized and tested in vitro for their inhibitory activities. The most promising...
The paper describes synthesis and comparative study on antibacterial activities of sulphonamides and Mannich bases derived from them. The compounds were screened for their antibacterial activity against various gram-positive and gram-negative bacteria and were analyzed statistically. The results...
Synthesis of phosphonooxymethyl derivatives of ravuconazole, 2 (BMS-379224) and 3 (BMS-315801) and their biological evaluation as potential water-soluble prodrugs of ravuconazole are described. The phosphonooxymethyl ether analogue 2 (BMS-379224) and N -phosphonooxymethyl triazolium salt 3...
As part of our ongoing program to explore novel structural classes of FKBP12 ligands, we herein wish to report a new class of FKBP12 ligands containing chiral bicyclic proline analogues. Details of the synthetic routes, together with preliminary biological activity, will be presented.
Thioacetal artemisinin derivatives, in particular, 10α-phenylthiodihydroartemisinins ( 5 ), 10β-benzenesulfonyl-9- epi -dihydroartemisinin ( 9 ) and 10α-mercaptodihydroartemisinin ( 11 ), exhibit good growth inhibition activity against HUVEC proliferation at the concentration level of 1 μM.
Compounds having methyl, vinyl, and ethynyl groups at the 4′-position of stavudine (d4T: 2′,3′-didehydro-3′-deoxythymidine) were synthesized. The compounds were assayed for their ability to inhibit the replication of HIV in cell culture. The 4′-ethynyl analogue ( 15 ) was found to be...
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