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At least 595 records · Page 33Linked to original sources
PubMed2005

Two new chiral nucleoside analogues: (4R,5R)-4-(4,6-dimethylpyrimidin-2-ylsulfanyl)-5-[(2S,5R)-2-isopropyl-5-methylcyclohexyloxy]-2,3,4,5-tetrahydrofuran-2-one and (4R,5R)-5-[(2S,5R)-isopropyl-5-methylcyclohexyloxy]-4-(4-methyl-1,3-thiazol-2-ylamino)-2,3,4,5-tetrahydrofuran-2-one.

Synthesis and X-ray structural investigations have been carried out for the two title compounds, viz. C20H30N2O3S, (I), and C18H28N2O3S, (II). In both molecules, the cyclohexyloxy moiety and the conjugated cyclic system are located on opposite sides of the tetrahydrofuran-2-one ring. In the crystal structure of (II), there are two types of intermolecular hydrogen bonds, viz. C-H...S and N-H...O, and the molecules form a three-dimensional supramolecular architecture via the hydrogen bonds.

Crystallography, X-Ray↗
PubMed1993

Biological evaluation of compounds with -NCS- group or derived from thiazole and imidazole. Activity on prostaglandin synthetase complex.

The effects of compounds with activity against thyroid peroxidase were tested on the activity of hydroperoxidase and cyclo-oxygenase of the prostaglandin synthetase complex in-vitro. Active compounds were found to inhibit the peroxidase, and the cyclo-oxygenase function. These compounds were also found to have anti-inflammatory activity as demonstrated by the reduction of carrageenan-induced oedema of the hind paw of the rat. Indomethacin and non-steroidal anti-inflammatory drugs tested under the same conditions were shown to have activity towards the cyclo-oxygenase rather than the peroxidase function of the prostaglandin synthetase complex. A common feature of the active compounds was the presence of an -NCS- linkage or free -SH group.

Animals↗
PubMed2004

Antimicrobial evaluation of nocathiacins, a thiazole peptide class of antibiotics.

Nocathiacins are cyclic thiazolyl peptides with inhibitory activity against gram-positive bacteria. BMS-249524 (nocathiacin I), identified from screening a library of compounds against a multiply antibiotic-resistant Enterococcus faecium strain, was used as a lead chemotype to obtain additional structurally related compounds. The MIC assay results of BMS-249524 and two more water-soluble derivatives, BMS-411886 and BMS-461996, revealed potent in vitro activities against a variety of gram-positive pathogens including methicillin-resistant Staphylococcus aureus, penicillin-resistant Streptococcus pneumoniae, vancomycin intermediate-resistant S. aureus, vancomycin-resistant enterococci, Mycobacterium tuberculosis and Mycobacterium avium. Analysis of killing kinetics revealed that these compounds are bactericidal for S. aureus with at least a 3-log(10) reduction of bacterial growth within 6 h of exposure to four times the MICs. Nocathiacin-resistant mutants were characterized by DNA sequence analyses. The mutations mapped to the rplK gene encoding the L11 ribosomal protein in the 50S subunit in a region previously shown to be involved in the binding of related thiazolyl peptide antibiotics. These compounds demonstrated potential for further development as a new class of antibacterial agents with activity against key antibiotic-resistant gram-positive bacterial pathogens.

Anti-Bacterial Agents↗