- Preparation and application of guaifenazulene aldole dicondensate (by machine translation)
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The invention belongs to the field, and particularly relates to chemical preparation and application. When the problem group is subjected to chemical synthesis research on the skeleton by guaiguazulene and piperidine acid as raw materials, the derivative trans - 1, 2 - (1, 4 - diazulyl) ethene ene derivative of guaiabazulene is found. H1N1 Influenza virus testing, indicating that the compound is level, 25 mm in vitro antiviral activity superior to that of positive drug ribavirin. In vivo activity tests prove, the compound not only can inhibit the pneumonia symptoms, but also can reduce the titer, and the survival rate. , The survival rate, 5 mg/kg/day the lung virus titer . of virus-infected mice can be remarkably improved when stomach tube-like dosages are used for gastric lavage. In general, the activity of the compound is comparable, and the activity of the compound is comparable to that of oseltamivir. The utility model can be used for preparing antiviral drugs. The invention opens up a new way for deep research and development of new antiviral drugs, which is a new approach. (by machine translation)
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Paragraph 0019; 0020
(2019/08/02)
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- Metalloporphyrin dimers bridged by a peptoid helix: Host-guest interaction and chiral recognition
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Co-facial porphyrins have been designed to construct porphyrin tweezers with versatile molecular recognition capabilities. In this study, we synthesized metalloporphyrin-peptoid conjugates (MPPCs) displaying two metalloporphyrins on a peptoid scaffold with either achiral unfolded (1) or helical (2 and 3) secondary structures. Host-guest complexation of MPPCs was realized with various guests of different lengths and basicities, and the extent of complexation was measured by UV-vis and circular dichroism (CD) spectroscopic titration. Intermolecular and intramolecular chirality induction were observed on achiral and chiral peptoid backbones, respectively. Spectroscopic data indicated that a broad scope of achiral guests can be recognized by chiral 2; in particular, longer and more flexible guests were seen to bind more tightly on 2. In addition, chiral 2 provided a distinct CD couplet with DL-, D-, or L-Lys-OMe, which was a result of the diastereomeric host-guest complex formation. Our results indicated that MPPCs can recognize, contrast, and analyze various achiral, chiral, or racemic molecules. Based on co-facial metalloporphyrins present on peptoid scaffolds, we developed a novel class of porphyrin tweezers, which can be further utilized in asymmetric catalysis, molecular sensing, and drug delivery.
- Lee, Yen Jea,Kang, Boyeong,Seo, Jiwon
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- Method for preparing amino-acid ester
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The invention relates to a method for preparing an amino-acid ester and belongs to the field of organic compound synthesis. The method comprises the following steps: by taking sulfur trioxide as a catalyst and a water bounding agent, catalyzing amino acid to react with an alcohol so as to prepare sulfate of the amino-acid ester, concentrating the reaction system, removing a reaction solvent, dissolving with water, and further neutralizing with ammonia water, thereby obtaining the amino-acid ester. The method for preparing the amino-acid ester, which is provided by the technical scheme of the invention, has the advantages of being gentle in reaction process, high in yield, high in purity, simple to operate and low in cost. By adopting the method for preparing the amino-acid ester, centrifugal mother liquid condensed water can be subjected to biochemical treatment directly, a solid byproduct of high-purity ammonium sulfate can be generated, the byproduct can be used as a chemical fertilizer, the reaction process is green and pollution-free, and the environment can be protected.
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Paragraph 0023
(2018/12/03)
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- Comparison of liquid chromatography-isotope ratio mass spectrometry (LC/IRMS) and gas chromatography-combustion-isotope ratio mass spectrometry (GC/C/IRMS) for the determination of collagen amino acid δ13C values for palaeodietary and palaeoecological reconstruction
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Results are presented of a comparison of the amino acid (AA) δ13C values obtained by gas chromatography-combustion-isotope ratio mass spectrometry (GC/C/IRMS) and liquid chromatography-isotope ratio mass spectrometry (LC/IRMS). Although the primary focus was the compound-specific stable carbon isotope analysis of bone collagen AAs, because of its growing application for palaeodietary and palaeoecological reconstruction, the results are relevant to any field where AA δ13C values are required. We compare LC/IRMS with the most up-to-date GC/C/IRMS method using N-acetyl methyl ester (NACME) AA derivatives. This comparison involves the analysis of standard AAs and hydrolysates of archaeological human bone collagen, which have been previously investigated as N-trifluoroacetyl isopropyl esters (TFA/IP). It was observed that, although GC/C/IRMS analyses required less sample, LC/IRMS permitted the analysis of a wider range of AAs, particularly those not amenable to GC analysis (e.g. arginine). Accordingly, reconstructed bulk δ13C values based on LC/IRMS-derived δ13C values were closer to the EA/IRMS-derived δ13C values than those based on GC/C/IRMS values. The analytical errors for LC/IRMS AA δ13C values were lower than GC/C/IRMS determinations. Inconsistencies in the δ13C values of the TFA/IP derivatives compared with the NACME- and LC/IRMS-derived δ13C values suggest inherent problems with the use of TFA/IP derivatives, resulting from: (i) inefficient sample combustion, and/or (ii) differences in the intra-molecular distribution of δ13C values between AAs, which are manifested by incomplete combustion. Close similarities between the NACME AA δ13C values and the LC/IRMS-derived δ13C values suggest that the TFA/IP derivatives should be abandoned for the natural abundance determinations of AA δ13C values.
- Dunn, Philip J. H.,Honch, Noah V.,Evershed, Richard P.
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experimental part
p. 2995 - 3011
(2012/05/20)
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- Two-component dendritic gel: Effect of stereochemistry on the supramolecular chiral assembly
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The self-assembly of diaminododecane solubilised by four different stereoisomeric dendritic peptides to form gel-phase materials in toluene was investigated. The second generation dendritic peptides were based on D- and L-lysine building blocks, and each contained three chiral centres. By designing dendritic peptides in which the configurations of the chiral centres were modified, and applying them as gelator units, the assembly of stereoisomers could be investigated. In all cases, the self-assembly of gelator units resulted in macroscopic gelation. However, the degree of structuring was modulated by the stereoisomers employed, an effect which changed the morphology and macroscopic behavior of the self-assembled state. Enantiomeric (L,L,L or D,D,D) gelator units formed fibrous molecular assemblies, whilst the racemic gel (50% L,L,L: 50% D,D,D) formed a flat structure with a "woven" appearance. Gelator units based on L,D,D or D,L,L dendritic peptides also formed fibrous assemblies, but small-angle X-ray scattering indicated significant morphological differences were caused by the switch in chirality. Furthermore, the macroscopic stability of the gel was diminished when these peptides were compared with their L,L,L or D,D,D analogues. In this paper it is clearly shown that individual stereocentres, on the molecular level, are directly related to the helicity within the fibre. It is argued that the chirality controls the pattern of hydrogen bonding within the assembly, and hence determines the extent of fibre formation and the macroscopic gel strength.
- Hirst, Andrew R.,Smith, David K.,Feiters, Martin C.,Geurts, Huub P. M.
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p. 5901 - 5910
(2007/10/03)
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- Long-wavelength water soluble chlorin photosensitizers useful for photodynamic therapy and diagnosis of tumors
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Novel photosensitizers useful for photodynamic therapy and diagnosis of tumors. Photosensitizers are derived from chlorophyll-a of photosynthetic plants and algae, possess long wavelength absorption between 600 and 800 nm, are stable, and water soluble. A process of preparation of these compounds and method of use for diagnostic and therapeutic purposes.
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