- BETA ADRENERGIC AGONIST AND METHODS OF USING THE SAME
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The present disclosure is directed to chemical compounds and to the use of such compounds in the treatment of diseases associated with an adrenergic receptor. In certain embodiments of the methods disclosed herein, the methods include administering to the subject a compound as disclosed herein and a peripherally acting P-blocker (PABRA).
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- Turning Cucurbit[8]uril into a Supramolecular Nanoreactor for Asymmetric Catalysis
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Chiral macromolecules have been widely used as synthetic pockets to mimic natural enzymes and promote asymmetric reactions. An achiral host, cucurbit[8]uril (CB[8]), was used for an asymmetric Lewis acid catalyzed Diels-Alder reaction. We achieved a remarkable increase in enantioselectivity and a large rate acceleration in the presence of the nanoreactor by using an amino acid as the chiral source. Mechanistic and computational studies revealed that both the amino acid-Cu2+ complex and the dienophile substrate are included inside the macrocyclic host cavity, suggesting that contiguity and conformational constraints are fundamental to the catalytic process and rate enhancement. These results pave the way towards new studies on asymmetric reactions catalyzed in confined achiral cavities.
- Zheng, Lifei,Sonzini, Silvia,Ambarwati, Masyitha,Rosta, Edina,Scherman, Oren A.,Herrmann, Andreas
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supporting information
p. 13007 - 13011
(2015/11/02)
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- Effects of structural modifications on the metal binding, anti-amyloid activity, and cholinesterase inhibitory activity of chalcones
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As the number of individuals affected with Alzheimer's disease (AD) increases and the availability of drugs for AD treatment remains limited, the need to develop effective therapeutics for AD becomes more and more pressing. Strategies currently pursued include inhibiting acetylcholinesterase (AChE) and targeting amyloid-β (Aβ) peptides and metal-Aβ complexes. This work presents the design, synthesis, and biochemical evaluation of a series of chalcones, and assesses the relationship between their structures and their ability to bind metal ions and/or Aβ species, and inhibit AChE/BChE activity. Several chalcones were found to exhibit potent disaggregation of pre-formed N-biotinyl Aβ1-42 (bioAβ42) aggregates in vitro in the absence and presence of Cu2+/Zn2+, while others were effective at inhibiting the action of AChE.
- Fosso, Marina Y.,LeVine, Harry,Green, Keith D.,Tsodikov, Oleg V.,Garneau-Tsodikova, Sylvie
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supporting information
p. 9418 - 9426
(2015/09/15)
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- Volatile compounds formed from the pyrolysis of chitosan
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Chitosan is a renewable resource for the production of nitrogen-containing aromatic heterocyclics. It was found that chitosan started to decompose and produce some volatile compounds at around 525 K in a nitrogen atmosphere, the volatiles were characterized by Fourier transform infrared spectrometer. The apparent activation energy for the thermal degradation of chitosan was determined. To further investigate the degradation, chitosan was pyrolyzed under vacuum at 553 K for 1 h, and the volatile compounds were analyzed by gas chromatography/mass spectrometry. The volatile compounds included aromatic heterocyclics such as pyrazines, pyridines, pyrroles and furans, and the pyrazines were the major products. The pyrolysis mechanism of chitosan was also proposed.
- Zeng, Lintao,Qin, Caiqin,Wang, Liansheng,Li, Wei
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experimental part
p. 1553 - 1557
(2011/09/14)
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- Compounds with Bridgehead Nitrogen
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The position of conformational equilibra in 1,5-,1,6- and 1,8-dimethylperhydro-oxazolopyridines were determined by 1H NMR spectroscopy.The cis-(H-5,H-8a)-1,5-dimethylperhydro-oxazolopyridines adopted the trans fused conformation, as did the two isomers of cis-(H-1,H-8a)-1,6-dimethyl-perhydro-oxazolopyridine.In contrast, r-1,t-6,t-8a-1,6-dimethyl-perhydro-oxazolopyridine preferred the cis-fused conformation.Three of the 1,8-dimehylperhdro-oxazolopyridines adopted the trans-fused conformations (with distortion of the system in the case of the r-1,c-8,c-8a derivative) and the r-1,c-8,c-8a-1,8-dimethyl derivative adopted the cis-fused conformation.
- Crabb, Trevor A.,Heywood, Geoffrey C.
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p. 242 - 248
(2007/10/02)
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