17791-52-5Relevant articles and documents
An improved synthesis of tert butyloxycarbonyl L histidine
Van Batenburg,Kerling
, p. 1 - 2 (1976)
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Mechanically Strong Heterogeneous Catalysts via Immobilization of Powderous Catalysts to Porous Plastic Tablets
Li, Tingting,Xu, Bo
supporting information, p. 2673 - 2678 (2021/08/03)
Main observation and conclusion: We describe a practical and general protocol for immobilization of heterogeneous catalysts to mechanically robust porous ultra-high molecular weight polyethylene tablets using inter-facial Lifshitz-van der Waals Interactions. Diverse types of powderous catalysts, including Cu, Pd/C, Pd/Al2O3, Pt/C, and Rh/C have been immobilized successfully. The immobilized catalysts are mechanistically robust towards stirring in solutions, and they worked well in diverse synthetic reactions. The immobilized catalyst tablets are easy to handle and reused. Moreover, the metal leaching of immobilized catalysts was reduced significantly.
Synthesis method of N alpha-tert-butyloxycarbonyl-L-histidine
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Paragraph 0030; 0032-0033; 0035-0036; 0038-0039; 0041, (2020/09/09)
The invention relates to a synthesis method of N alpha-tert-butyloxycarbonyl-L-histidine, which comprises the following steps of: dissolving solid L-histidine in a sodium carbonate water solution, dropwisely adding liquid di-tert-butyl dicarbonate, reacting, filtering, and washing the filtrate with an organic solvent to remove unreacted di-tert-butyl dicarbonate; after the reaction solution is subjected to aqueous phase acidification, adding an extracting agent ethyl acetate for extraction, conducting standing and layering, and washing, drying and filtering an oil phase to obtain an ethyl acetate solution containing an intermediate N alpha-tert-butyloxycarbonyl-Nim-tert-butyloxycarbonyl-L-histidine; stirring the ethyl acetate solution containing the intermediate N alpha-tert-butyloxycarbonyl-Nim-tert-butyloxycarbonyl-L-histidine at 50-100 DEG C for reaction, and after the reaction is finished, carrying out after-treatment to obtain the product N alpha-tert-butyloxycarbonyl-L-histidine.The synthesis method of N alpha-tert-butyloxycarbonyl-L-histidine provided by the invention is simple in process and convenient to operate, the product purity and yield are higher than those in the prior art, the technical problem that purification and desalination are not thorough by using ion exchange resin is solved, and the synthesis method is suitable for industrial production.
Discovery of a Membrane-Active, Ring-Modified Histidine Containing Ultrashort Amphiphilic Peptide That Exhibits Potent Inhibition of Cryptococcus neoformans
Sharma, Krishna K.,Maurya, Indresh Kumar,Khan, Shabana I.,Jacob, Melissa R.,Kumar, Vinod,Tikoo, Kulbhushan,Jain, Rahul
, p. 6607 - 6621 (2017/08/17)
The new structural classes of ultrashort peptides that exhibit potent microbicidal action have potential as future drugs. Herein, we report that C-2 arylated histidines containing tripeptides His(2-Ar)-Trp-His(2-Ar) exhibit potent antifungal activity against Cryptococcus neoformans with high selectivity. The most potent peptide 12f [His(2-biphenyl)-Trp-His(2-biphenyl)] displayed high in vitro activity against C. neoformans (IC50 = 0.35 μg/mL, MIC = MFC = 0.63 μg/mL) with a selectivity index of >28 and 2 times higher potency compared to amphotericin B. Peptide 12f exhibited proteolytic stability, with no apparent hemolytic activity. The mechanism of action study of 12f by confocal laser scanning microscopy and electron microscopy indicates nuclear fragmentation and membrane disruption of C. neoformans cells. Combinations of 12f with fluconazole and amphotericin B at subinhibitory concentration were synergistic against C. neoformans. This study suggests that 12f is a new structural class of amphiphilic peptide with rapid fungicidal activity caused by C. neoformans.
