6630-04-2Relevant academic research and scientific papers
Modulation of Bambusuril Anion Affinity in Water
Havel, Vaclav,Babiak, Michal,Sindelar, Vladimir
supporting information, p. 8963 - 8968 (2017/07/11)
Neutral and negatively charged anion receptors functioning in pure water are rare in supramolecular chemistry. Moreover, studies on adjusting the affinity of such receptors toward anions in water are absent from the literature. Two new bambusurils, 1 a and 2 a, were prepared to demonstrate that the affinity of bambusurils towards anions can be altered by the length of carboxyalkyl groups attached to the macrocycles. The stability of the bambusuril complexes was further controlled by the pH value. The crystal structure of bambusuril 1 a was described, in which two carboxyalkyl arms fold into the macrocycle cavity, thus forming the intramolecular self-inclusion complex.
Novel symmetrical ureas as modulators of protein arginine methyl transferases
Fontán, Noelia,García-Domínguez, Patricia,álvarez, Rosana,De Lera, ángel R.
, p. 2056 - 2067 (2013/05/09)
Methylation of histone arginine residues is an epigenetic mark related to gene expression that is implicated in a variety of biological processes and can be reversed by small-molecule modulators of protein arginine methyltransferases (PRMTs). A series of symmetrical ureas, designed as analogues of the known PRMT1 inhibitor AMI-1 have been synthesized using Pd-catalyzed Ar-N amide bond formation processes or carbonylation reactions as key steps. Their inhibitory profile has been characterized. The enzymatic assays showed a weak effect on PRMT1 and PRMT5 activity for most of the compounds. The acyclic urea that exhibited the strongest effect on the inhibition of the PRMT1 activity also showed the greatest effect on the expression of some androgen receptor target genes (TMPRSS2 and FKBP5), which may be related with its enzymatic activity. Surprisingly, AMI-1 behaved as an activator of PRMT5 activity, a result not reported so far.
Urea and thiourea compounds and compositions for cholesterol management and related uses
-
Page/Page column 70, (2010/02/13)
The present invention relates to novel urea and thiourea compounds, compositions comprising urea or thiourea compounds, and methods useful for treating and preventing aging, Alzheimer's Disease, cancer, cardiovascular disease, diabetic nephropathy, diabetic retinopathy, a disorder of glucose metabolism, dyslipidemia, dyslipoproteinemia, enhancing bile production, enhancing reverse lipid transport, hypertension, impotence, inflammation, insulin resistance, lipid elimination in bile, modulating C reactive protein, obesity, oxysterol elimination in bile, pancreatitis, Parkinson's disease, a peroxisome proliferator activated receptor-associated disorder, phospholipid elimination in bile, renal disease, septicemia, metabolic syndrome disorders (e.g., Syndrome X), a thrombotic disorder, gastrointestinal disease, irritable bowel syndrome (IBS), inflammatory bowel disease (e.g., Crohn's Disease, ulcerative colitis), arthritis (e.g., rheumatoid arthritis, osteoarthritis), autoimmune disease (e.g., systemic lupus erythematosus), scleroderma, ankylosing spondylitis, gout and pseudogout, muscle pain: polymyositis/polymyalgia rheumatica/fibrositis; infection and arthritis, juvenile rheumatoid arthritis, tendonitis, bursitis and other soft tissue rheumatism. In certain embodiments, the compounds, compositions, and methods of the invention are useful in combination therapy with other therapeutics, such as hypocholesterolemic and hypoglycemic agents.
Molecular symmetry and the design of molecular solids: The oxalamide functionality as a persistent hydrogen bonding unit
Coe, Seth,Kane, John J.,Nguyen, Tam Luong,Toledo, Leticia M.,Wininger, Eric,Fowler, Frank W.,Lauher, Joseph W.
, p. 86 - 93 (2007/10/03)
A symmetry analysis based upon the structure of simple molecules and their anticipated intermolecular interactions can lead to successful predictions of molecular packing and crystal symmetry. As a demonstrated of these ideas an in-depth study of the oxalamide functionality as a persistent hydrogen bonding unit is presented. The synthesis and structural characterization of a series oxalamide dicarboxylic acids is presented and the structures compared with the analogous urea compounds. Both the urea and oxalamide dicarboxylic acids form designed two-dimensional hydrogen-bonded β-networks with a significant degree of reliability. The urea designs are quite reliable when there is a molecular 2-fold axis, but competing hydrogen bond patterns are found when less symmetrical molecules are studied. The oxalamide design based on inversion centers is also quite reliable, with the designed layer structure found in most cases.
