87052-59-3Relevant academic research and scientific papers
Preparation method of water-soluble florfenicol amino acid salt
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Paragraph 0077; 0084-0085, (2020/07/21)
The invention discloses a preparation method of a water-soluble florfenicol amino acid ester salt. The method comprises the following steps: using florfenicol and N-Cbz-amino acid as the initial raw materials, carrying out acylating chlorination, esterifi
Discovery of simplified leucyladenylate sulfamates as novel leucyl-tRNA synthetase (LRS)-targeted mammalian target of rapamycin complex 1 (mTORC1) inhibitors
Yoon, Suyoung,Kim, Jong Hyun,Koh, Yura,Tran, Phuong-Thao,Ann, Jihyae,Yoon, Ina,Jang, Jayun,Kim, Won Kyung,Lee, Sangkook,Lee, Jiyoun,Kim, Sunghoon,Lee, Jeewoo
, p. 4145 - 4152 (2017/07/05)
Leucyl-tRNA synthetase (LRS) has been reported to be a possible mediator of intracellular amino acids signaling to mTORC1. Given that mTORC1 is associated with cell proliferation and tumorigenesis, the LRS-mediated mTORC1 pathway may offer an alternative
Structural optimization of azadipeptide nitriles strongly increases association rates and allows the development of selective cathepsin inhibitors
Frizler, Maxim,Lohr, Friederike,Furtmann, Norbert,Kl?s, Julia,Gütschow, Michael
supporting information; experimental part, p. 396 - 400 (2011/03/18)
Using the example of cathepsin K, we demonstrate the design of highly potent and selective azadipeptide nitrile inhibitors. A systematic scan with respect to P2 and P3 substituents was carried out. Structural modifications strongly affected the enzyme-inh
Amino acid amides of 2-benzimidazole as acid-stable prodrugs of potential inhibitors of H+/K+ ATPase
Hirai, K,Koike, H,Ishiba, T,Ueda, S,Makino, I,et al.
, p. 143 - 158 (2007/10/02)
A series of amino acid amides of 2-benzimidazole were prepared and found to possess gastric antisecretory activity on oral administration. (Glycylaminobenzyl)sulfinyl compound 23a, stable in artificial gastric juice (pH 1.2), was given orally to dogs.It was absorbed efficiently and converted into aniline derivative 7a which showed a very high plasma concentration.Compound 23a was hydrolyzed by the action of aminopeptidase present in plasma or the brush border fraction of the small intestine to release the terminal glycine. o-Aniline derivatives showed good activity in in vitro H+/K+-ATPase inhibition as well as in the inhibition of histamine stimulated acid secretion in isolated bullfrog gastric mucosa.Although these o-aniline derivatives showed no or weak gastric antisecretory activity in rat by id administration, they were active when administered ip.Therefore, these amino acid amides were considered to be acid stable prodrugs of proton pump inhibiting o-aniline derivatives.The mechanism of H+/K+-ATPase inhibition of 7a was also examined.
Amino Acids and Peptides; 67. Easy Preparation and Use of Benzyloxycarbonyl Derivatives of Amino Acid Chlorides and α-Hydroxycarboxylic Acid Chlorides
Schmidt, Ulrich,Kroner, Matthias,Beutler, Ulrich
, p. 475 - 477 (2007/10/02)
N-Benzyloxycarbonyl amino acid chlorides and α-benzyloxycarbonyloxy carboxylic acid chlorides are readily available by treating the corresponding carboxylic acids with 1-chloro-N,N,2-trimethyl-1-propen-1-amine.They can be immediately reacted with O-, N- and C-nucleophiles to afford peptides, ketones and esters.
