645-72-7Relevant articles and documents
Comparison of the supramolecular structures of two glyco lipids with chiral and nonchiral methyl-branched alkyl chains from natural sources
Milkereit, G?tz,Garamus, Vasil M.,Yamashita, Jun,Hato, Masakatsu,Morr, Michael,Vill, Volkmar
, p. 1599 - 1608 (2005)
Two alkyl glycosides with the same type of disaccharide headgroups (melibiose) and different methyl-branched alkyl chains, short chiral [(2R,4R,6R,8R)-2,4,6,8-tetramethyldecyl, extracted from an animal source] and long nonchiral (3,7,11,15-tetramethylhexadecyl, from a plant source), were synthesized. The supramolecular aggregate structure formed in dilute solutions was investigated by small-angle neutron scattering and surface tension measurements. The lyotropic phase diagram was studied by differential scanning calorimetry and water penetration scans. The thermotropic phase behavior was investigated by polarizing microscopy. The compounds showed unusual phase behavior: (i) The liquid-crystalline polymorphism is reduced to only form smectic A phases in the pure state; the formation of lyotropic phases such as hexagonal or lamellar phases was not observed, (ii) The compound with the longer nonchiral alkyl chain is more soluble in water than the one with the shorter chiral chain, most likely because of the different flexibilities of the chains, (iii) For the long-chain compound, the formation of micelles is observed, whereas the short-chain compound forms large disklike/bilayer aggregates. The method of methylation of the chain controls the self-assembly and can explain different biological functions for either plants (variable temperature) or animals (constant temperature).
Phosphoramidite reagent and applications thereof in oligonucleotide synthesis
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Paragraph 0198; 0201; 0202, (2020/05/02)
The invention provides a phosphoramidite reagent and applications thereof. According to the invention, the phosphoramidite reagent is a 2-nitrile ethoxy phosphoramidite compound with a large non-polarsubstituent group on a 2-nitrile ethoxy group, and can react with a nucleoside monomer or a nucleotide fragment 3'-OH or 5'-OH to generate phosphoramidite diester, the phosphoramidite diester continuously reacts with another group of nucleoside monomers or nucleotide fragments 3'-OH or 5'-OH under the action of a proper activating agent to generate phosphoramidite trimester, oxidizing or vulcanizing is performed to obtain phosphoric acid triester or thiophosphoric acid trimester, and deprotection is performed to obtain oligonucleotides, wherein in the whole process, all phosphite intermediates or phosphate intermediates are easily dissolved in a solvent with medium and low polarity and have low solubility in a high-polar solvent while other reaction raw materials or by-products are easilydissolved in the high-polar solvent, such that the purification can be performed through non-polar/polar solvent extraction so as not to hinder the subsequent chain propagation reaction; the method is suitable for one-by-one nucleotide linking and reactions linked by a fragment method.
Discovery of Lipophilic Bisphosphonates That Target Bacterial Cell Wall and Quinone Biosynthesis
Malwal, Satish R.,Chen, Lu,Hicks, Hunter,Qu, Fiona,Liu, Weidong,Shillo, Alli,Law, Wen Xuan,Zhang, Jianan,Chandnani, Neal,Han, Xu,Zheng, Yingying,Chen, Chun-Chi,Guo, Rey-Ting,Abdelkhalek, Ahmed,Seleem, Mohamed N.,Oldfield, Eric
supporting information, p. 2564 - 2581 (2019/03/07)
We report that alkyl-substituted bisphosphonates have activity against Bacillus anthracis Sterne (0.40 μg/mL), Mycobacterium smegmatis (1.4 μg/mL), Bacillus subtilis (1.0 μg/mL), and Staphylococcus aureus (13 μg/mL). In many cases, there is no effect of serum binding, as well as low activity against a human embryonic kidney cell line. Targeting of isoprenoid biosynthesis is involved with 74 having IC50 values of ～100 nM against heptaprenyl diphosphate synthase and 200 nM against farnesyl diphosphate synthase. B. subtilis growth inhibition was rescued by addition of farnesyl diphosphate, menaquinone-4 (MK-4), or undecaprenyl phosphate (UP), and the combination of MK-4 and UP resulted in a 25× increase in ED50, indicating targeting of both quinone and cell wall biosynthesis. Clostridioides difficile was inhibited by 74, and since this organism does not synthesize quinones, cell wall biosynthesis is the likely target. We also solved three X-ray structures of inhibitors bound to octaprenyl diphosphate and/or undecaprenyl diphosphate synthases.
COMPOSITIONS SOUS FORME D'UNE SOLUTION AQUEUSE INJECTABLE COMPRENANT DU GLUCAGON HUMAIN ET UN CO-POLYAMINOACIDE
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Paragraph 1233-1236, (2019/09/20)
Physically stable compositions in the form of an injectable aqueous solution, wherein the pH is from 6.0 to 8.0, includes at least: a) human glucagon andb) a co-polyamino acid bearing carboxylate charges and hydrophobic radicals Hy. In one embodiment, the compositions further comprise a gut hormone.
