cas 88321-09-9, Aloxistatin | Articles data ｜lookchem

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88321-09-9

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COMPOSITIONS AND METHODS FOR SYNTHESIZING (2S,3S)-TRANS-EPOXYSUCCINYL-L-LEUCYL-AMIDO-3-METHYLBUTANE ETHYL ESTER
In alternative embodiments the invention provides methods for synthesizing AB-007 (also called loxistatin, E64d, EST or ((2S,3S)-trans-epoxysuccinyl-L-leucyl-amido-3-methylbutane ethyl ester) and its acid form E64c (loxistatin acid), and various synthetic
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Paragraph 0057

(2017/07/06)

Design, synthesis, and screen of cathepsin K inhibitors
We synthesized a series of epoxysuccinic acid derivatives and evaluated their in vitro cathepsin K inhibitory activity The screening results show that the potency of compounds 9e, 9d, 9p, 9j and 9k (IC50 ≤ 0.005 μmol/L) were equal to or greater than that of the lead compound 9a. Less hydrophobic compounds showed weaker potency, which can be explained by the hydrophobic nature of the cathepsin K binding pockets.
Yu, Ying-Ying,Sun, Wei,Dong, Lei,Liu, Hai-Dong,Jiang, Dan,Xiao, Jun-Hai,Yang, Xiao-Hong,Li, Song
p. 715 - 718
(2013/07/26)

Stereoselective synthesis of the epoxysuccinyl peptide E-64c
A highly diastereoselective PTC epoxidation is employed in the synthesis of the potent cysteine protease inhibitor E-64c. Georg Thieme Verlag Stuttgart.
Lygo, Barry,Gardiner, Stuart D.,To, Daniel C. M.
p. 2063 - 2066
(2008/02/05)

A new synthesis of peptidyl epoxysuccinates for probing cysteine protease-inhibitor P3/S3 binding interactions
A new synthesis of peptidyl epoxysuccinates has been developed involving the N-acylation of amino acid benzyl esters (12) with the tartrate ester derived epoxy acid 13 followed by deprotection of the benzyl esters and acylation with amines 21-28. This syn
Roush, William R.,Hernandez, Alejandro Alvarez,Zepeda, Gerardo
p. 1500 - 1504
(2007/10/03)

Mechanistic studies on the inactivation of papain by epoxysuccinyl inhibitors
Analogs of the epoxysuccinyl peptide cysteine proteinase inhibitor, EP- 475 (2a), in which the free carboxylate has been replaced by hydroxamic acid, amide, methyl ketone, hydroxyl, and ethyl ester functionalities, have been synthesized. Individual rate c
Meara, Joseph P.,Rich, Daniel H.
p. 3357 - 3366
(2007/10/03)

Efficient synthetic method for ethyl (+)-(2S,3S)-3-[(S)-3-methyl-1-(3-methylbutylcarbamoyl)butylcarbam oyl]-2-oxiranecarboxylate (EST), a new inhibitor of cysteine proteinases
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Tamai,Yokoo,Murata,Oguma,Sota,Sato,Kanaoka
p. 1098 - 1104
(2007/10/02)

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Chemical Properties

Melting Point: 126.2°C
Boiling Point: 538°C at 760 mmHg
Flash Point:279.2°C
Density: 1.102g/cm³
Solubility:Soluble in DMSO, DMF or ethanol
Storage Temp.:−20°C
Vapor Pressure: 1.2E-11mmHg at 25°C
Refractive Index: 1.5800 (estimate)
PSA: 97.03000
LogP: 1.79190

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