142717-44-0Relevant articles and documents
Campestarenes: New building blocks with 5-fold symmetry
Nam, Seong,Ware, David C.,Brothers, Penelope J.
, p. 6460 - 6469 (2018)
Campestarene is a planar, shape-persistent macrocycle with 5-fold symmetry. A range of derivatives bearing peripheral functional groups suitable for generating supramolecular interactions has been designed and synthesised for potential applications in creating 2D quasicrystal molecular assemblies. The new campestarene derivatives bear ester, carboxylic acid, methoxy, bromo, 4-pyridyl, 4-cyanophenyl and 4-phenyl carboxylic acid groups, including further derivatives of the latter two bearing alkyl chains on the phenyl groups to improve solubility. The campestarene derivatives were prepared by reductive condensation of phenol precursors bearing nitro and formyl groups using Na2S2O4. The target functional groups were installed either by pre-cyclisation derivatisation or by synthesis of methoxy-substituted campestarene and subsequent derivatisation. The cyclisation reaction is tolerant of the functional groups introduced. The ten new campestarene derivatives were characterised by NMR spectroscopy and MALDI-TOF MS, although the poor solubility of some examples precluded their detailed characterisation.
Aggrecanase-2 inhibitors based on the acylthiosemicarbazide zinc-binding group
Maingot, Lucie,Elbakali, Jamal,Dumont, Julie,Bosc, Damien,Cousaert, Nicolas,Urban, Agathe,Deglane, Gaelle,Villoutreix, Bruno,Nagase, Hideaki,Sperandio, Olivier,Leroux, Florence,Deprez, Benoit,Deprez-Poulain, Rebecca
, p. 244 - 261 (2013/10/01)
Osteoarthritis is a disabling disease characterized by the articular cartilage breakdown. Aggrecanases are potential therapeutic targets for the treatment of this pathology. At the starting point of this project, an acylthiosemicarbazide was discovered to inhibit aggrecanase-2. The acylthiosemicarbazide Zn binding group is also a convenient linker for library synthesis. A focused library of 920 analogs was thus prepared and screened to establish structure-activity relationships. The modification of the acylthiosemicarbazide was also explored. This strategy combining library design and discrete compounds synthesis yielded inhibitor 35, that is highly selective for aggrecanases over a panel of metalloproteases and inhibits the degradation of native fully glycosylated aggrecan. A docking study generated binding conformations explaining the structure-activity relationships.
PPAR AGONIST COMPOUNDS, PREPARATION AND USES
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Page/Page column 20, (2011/08/22)
The present invention relates to novel PPAR agonist compounds as well as pharmaceutical compositions containing them. The compounds according to the invention are of quite particular therapeutic interest, notably for treating diabetes and/or dyslipidemias, as well as for preventing cardiovascular pathologies.
COMPOUNDS WITH COMBINED CALCIUM CHANNEL BLOCKER AND β-ADRENERGIC ANTAGONIST OR PARTIAL AGONIST ACTIVITIES FOR TREATMENT OF HEART DISEASE
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Page/Page column 49-50, (2008/06/13)
The present invention provides compounds possessing inhibitory activity against β-adrenergic receptors and L-type calcium channels. The present invention further provides pharmaceutical compositions comprising such compounds, methods of preparing such compounds, and methods of using such compounds for regulating calcium homeostasis, for treating a disease, disorder or condition in which disregulation of calcium homeostasis is implicated, and for treating hypertension, cardiovascular disease, congestive heart failure, myocardial ischemia, cardiomyopathies, stroke or epilepsy.
Amidine compounds
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, (2008/06/13)
A compound of the formula [I] wherein R1, R2and R3are the same or different and each is hydrogen atom, wherein each symbol is as defined in the specification, a salt thereof or a prodrug thereof. The compound of the presen
Alkynyl containing hydroxamic acid compounds as matrix metalloproteinase and tace inhibitors
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Page column 38, (2008/06/13)
Compounds of the formula are useful in treating disease conditions mediated by TNF-α, such as rheumatoid arthritis, osteoarthritis, sepsis, AIDS, ulcerative colitis, multiple sclerosis, Crohn's disease and degenerative cartilage loss.
The Synthesis and Transition Temperatures of Novel Low Molar Mass Cholesteric Materials Derived from (R)-2-(4-Hydroxyphenoxy)propanoic Acid
Booth, Christopher J.,Gray, George W.,Toyne, Kenneth J.,Hardy, Judith
, p. 31 - 58 (2007/10/02)
A comprehensive series of (R)-2-(4-substituted-phenoxy)propanoates and (R)-2-(4-substituted-phenoxy)propanonitriles have been prepared.A wide variety of 4-substituents and ester functions have been examined to determine how the position of the chiral centre affects the cholesteric phase formation in these classes of materials; the synthesis of these novel materials, their transition temperatures and a procedure for assessing their optical purity are described and discussed.Mesogenicity is significantly depressed if the chiral centre is placed centrally within the molecule.
Aryloxyalkyl diketones
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, (2008/06/13)
Aryloxyalkyl diketones and keto-esters, useful as pesticidal and anti-viral agents, are prepared from an aryloxyalkyl halide and an alkali metal enolate salt of a diketone or keto-ester, or from a haloalkyl-diketone and an alkali metal salt of a phenol.
