166737-85-5Relevant academic research and scientific papers
Synthesis method of S-trityl-L-cysteinamide
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Paragraph 0007; 0013; 0015-0019, (2021/08/07)
The invention relates to a synthesis method of S-trityl-L-cysteinamide. The method mainly solves the technical problem of product racemization in the existing synthesis method. The preparation method comprises the following three steps: step 1, adding CDI into a tetrahydrofuran solution of (+)-S-trityl-L-cysteine, stirring to react for 4 hours, and adding ammonia water to obtain a compound 1; 2, the compound 1 reacts with piperidine in N, N-dimethylformamide to obtain a compound 2; and 3, dissolving the compound 2 in ethyl acetate, adding L-dibenzoyl tartaric acid to form salt, measuring that ee is greater than 99.0%, and alkalifying to obtain a pure compound 3.
Thiopeptide Pyridine Synthase TbtD Catalyzes an Intermolecular Formal Aza-Diels-Alder Reaction
Bogart, Jonathan W.,Bowers, Albert A.
supporting information, p. 1842 - 1846 (2019/01/30)
Thiopeptide pyridine synthases catalyze a multistep reaction involving a unique and nonspontaneous intramolecular aza-[4 + 2] cycloaddition between two dehydroalanines to forge a trisubstituted pyridine core. We discovered that the in vitro activity of pyridine synthases from the thiocillin and thiomuracin pathways are significantly enhanced by general base catalysis and that this broadly expands the enzymes substrate tolerance. Remarkably, TbtD is competent to perform an intermolecular cyclization in addition to its cognate intramolecular reaction, underscoring its versatility as a biocatalyst. These data provide evidence that pyridine synthases use a two-site substrate recognition model to engage and process their substrates.
Aminothiol compound, preparation method of aminothiol compound and application of aminothiol compound in radiation protection
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Paragraph 0079; 0083; 0084; 0085; 0119; 0123; 0124; 0125, (2017/04/03)
The invention discloses an aminothiol compound, a preparation method of the aminothiol compound and application of the aminothiol compound in radiation protection. The compound has a structure shown in the formula I in the description, wherein A1 is selected from -C(O)NR8-, -S(O)2-NR8-, -S(O)NR8- and -R7-NR8-, A2 is selected from carbonyl, sulfonyl, sulfinyl and substituted or unsubstituted C1-6 alkyl, R1, R2, R5 and R6 can be the same or not and are selected from hydrogen and substituted or unsubstituted C1-C5 alkyl or hetero alkyl, n is an integer from 0 to 20000, R3 and R4 are independently selected from hydrogen, X and substituted or unsubstituted C1-6 alkyl, X is selected from F, Cl, Br and I, R7 is selected from substituted or unsubstituted C1-C6 alkyl, and R8 is selected from hydrogen and substituted or unsubstituted C1-C6 alkyl. The compound has the effect of reducing biological injury caused by ionizing radiation and also has the effects of prolonging the lifetime of radiated animals and increasing the survival rate of the radiated animals.
CATHEPSIN CYSTEINE PROTEASE INHIBITORS
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Page/Page column 43-44, (2008/12/04)
The present invention relates to novel compounds of the formula (I), wherein R'-R7, X, Y, D and n are as defined in the specification. These compounds are cysteine protease inhibitors which include but are not limited to inhibitors of cathepsms K, L, S an
ACETYLENIC SULFONAMIDE THIOL TACE INHIBITORS
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Page 23, (2008/06/13)
Compounds of formula (B): (1a), or (1b), (1c) are provided wherein the variables are as defined herein which are useful in disease conditions mediated by TNF- alpha , such as rheumatoid arthritis, osteoarthritis, sepsis, AIDS, ulcerative colitis, multiple
Acetylenic sulfonamide thiol tace inhibitors
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, (2008/06/13)
The compounds of formula B: which are useful in disease conditions mediated by TNF-α, such as rheumatoid arthritis, osteoarthritis, sepsis, AIDS, ulcerative colitis, multiple sclerosis, Crohn's disease and degenerative cartilage loss
