150508-72-8Relevant academic research and scientific papers
Synthesis, structure, and SAR of tetrahydropyran-based LpxC inhibitors
Murphy-Benenato, Kerry E.,Olivier, Nelson,Choy, Allison,Ross, Philip L.,Miller, Matthew D.,Thresher, Jason,Gao, Ning,Hale, Michael R.
supporting information, p. A1213 - A1218 (2015/04/27)
In the search for novel Gram-negative agents, we performed a comprehensive search of the AstraZeneca collection and identified a tetrahydropyran-based matrix metalloprotease (MMP) inhibitor that demonstrated nanomolar inhibition of UDP-3-O-(acyl)-N-acetylglucosamine deacetylase (LpxC). Crystallographic studies in Aquifex aeolicus LpxC indicated the tetrahydropyran engaged in the same hydrogen bonds and van der Waals interactions as other known inhibitors. Systematic optimization of three locales on the scaffold provided compounds with improved Gram-negative activity. However, the optimization of LpxC activity was not accompanied by reduced inhibition of MMPs. Comparison of the crystal structure of the native product, UDP-3-O-(acyl)-glucosamine, in Aquifex aeolicus to the structure of a tetrahydropyran-based inhibitor indicates pathways for future optimization.
ASCORBATE, VITAMIN K3 AND HYDROXYTOLANS IN THE TREATMENT OF CANCER
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Page/Page column 21, (2009/01/23)
The combination of compounds of the hydroxytolan family with ascorbate plus naphthoquinone (Vitamin K3; VK3), or a quinone or semiquinone analogue of VK3, kill tumor cells, inhibit tumor growth and development, and treat cancer in subjects in need thereof.
Hydroxycruciforms: Amine-responsive fluorophores
McGrier, Psaras L.,Solntsev, Kyril M.,Miao, Shaobin,Tolbert, Laren M.,Miranda, Oscar R.,Rotello, Vincent M.,Bunz, Uwe H. F.
supporting information; experimental part, p. 4503 - 4510 (2009/05/08)
The synthesis of three hydroxy-substituted cruciforms (XF, 1,4-bis(4′-hydroxystyryl)-2,5-bis(4″-methoxyphenylethynyl)benzene, 1,4-bis(4′-methoxystyryl)-2,5-bis(4″-hydroxyphenylethynyl)benzene, and 1,4-bis(4′-hydroxystyryl)-2,5-bis(4″-hydroxyphenylethynyl)
Methods for treating subjects infected with a herpes virus or neisseria gonorrheae
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, (2008/06/13)
The present invention provides a method of inhibiting the formation of infectious herpes virus particles, particularly infectious herpes simplex virus (HSV) particles, in a host cell. The method involves administering an effective amount of a hydroxylated
Designing banana-shaped liquid crystals without Schiff's base units: m- Terphenyls, 2,6-diphenylpyridines and V-shaped tolane derivatives
Shen, Dong,Diele, Siegmar,Pelzl, Gerhard,Wirth, Ina,Tschierske, Carsten
, p. 661 - 672 (2007/10/03)
This paper reports attempts to obtain (anti)ferroelectric switchable achiral banana-shaped molecules without Schiff's base units. For this purpose we have synthesized novel V-shaped molecules consisting of rigid angular central units [1,3-disubstituted be
New chiral tolane series with antiferroelectric properties
Cluzeau,Nguyen,Destrade,Isaert,Barois,Babeau
, p. 69 - 91 (2007/10/02)
A new series of chiral tolane with aliphatic end chains ranging from heptyloxy to dodecyloxy has been synthesized and characterized. The mesomorphic properties have been analyzed by optical microscopy on pure compounds and mixtures, D.S.C, electro-optical
