5710-64-5Relevant academic research and scientific papers
Synthesis and Mesomorphic Properties of Novel Bent-shaped Naphthyl Diketones
Buljan, An?ela,Kne?evi?, Anamarija,Dokli, Irena,Lesac, Andreja
, p. 173 - 179 (2019/12/12)
The synthesis and liquid-crystalline properties are reported for novel naphthyl-based diketones incorporating variant terminal chains and lateral fluoro- substitution. Newly prepared materials exhibit a broad temperature range of the nematic phase. The study demonstrates how subtle structural modifications can be exploited to alter the efficiency of molecular packing and consequently the thermal behaviour.
Potent, novel in vitro inhibitors of the Pseudomonas aeruginosa deacetylase LpxC
Kline, Toni,Andersen, Niels H.,Harwood, Eric A.,Bowman, Jason,Malanda, Andre,Endsley, Stephanie,Erwin, Alice L.,Doyle, Michael,Fong, Susan,Harris, Alex L.,Mendelsohn, Brian,Mdluli, Khisimuzi,Raetz, Christian R. H.,Stover, C. Kendall,Witte, Pamela R.,Yabannavar, Asha,Zhu, Shuguang
, p. 3112 - 3129 (2007/10/03)
Deacetylation of uridyldiphospho-3-O-(R-hydroxydecanoyl)-N-acetylglucosamine by LpxC is the first committed step in the Pseudomonas aeruginosa biosynthetic pathway to lipid A; homologous enzymes are found widely among Gram-negative bacteria. As an essential enzyme for which no inhibitors have yet been reported, the P. aeruginosa LpxC represents a highly attractive target for a novel antibacterial drug. We synthesized several focused small-molecule libraries, each composed of a variable aromatic ring, one of four heterocyclic/spacer moieties, and a hydroxamic acid and evaluated the LpxC inhibition of these compounds against purified P. aeruginosa enzyme. To ensure that the in vitro assay would be as physiologically relevant as possible, we synthesized a tritiated form of the specific P. aeruginosa glycolipid substrate and measured directly the enzymatically released acetate. Several of our novel compounds, predominantly those having fluorinated substituents on the aromatic ring and an oxazoline as the heterocyclic moiety, demonstrated in vitro IC50 values less than 1 μM. We now report the synthesis and in vitro evaluation of these P. aeruginosa LpxC inhibitors.
