256390-71-3Relevant articles and documents
Convenient synthesis of L-proline benzyl ester
Cordova, Armando,Reed, Neal N.,Ashley, Jon A.,Janda, Kim D.
, p. 3119 - 3122 (1999)
Mesylates or tosylates of δ-hydroxy-L-norvaline esters spontaneously afford L-proline esters upon exposure to aqueous buffer in near quantitative yield. This novel reaction has led to the development of a simple route to optically active proline esters.
Synthesis and Evaluation of Oxyguanidine Analogues of the Cysteine Protease Inhibitor WRR-483 against Cruzain
Jones, Brian D.,Tochowicz, Anna,Tang, Yinyan,Cameron, Michael D.,McCall, Laura-Isobel,Hirata, Ken,Siqueira-Neto, Jair L.,Reed, Sharon L.,McKerrow, James H.,Roush, William R.
, p. 77 - 82 (2016)
A series of oxyguanidine analogues of the cysteine protease inhibitor WRR-483 were synthesized and evaluated against cruzain, the major cysteine protease of the protozoan parasite Trypanosoma cruzi. Kinetic analyses of these analogues indicated that they have comparable potency to previously prepared vinyl sulfone cruzain inhibitors. Co-crystal structures of the oxyguanidine analogues WRR-666 (4) and WRR-669 (7) bound to cruzain demonstrated different binding interactions with the cysteine protease, depending on the aryl moiety of the P1′ inhibitor subunit. Specifically, these data demonstrate that WRR-669 is bound noncovalently in the crystal structure. This represents a rare example of noncovalent inhibition of a cysteine protease by a vinyl sulfone inhibitor.
THIOPHOSPHATE NUCLEOSIDES FOR THE TREATMENT OF HCV
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, (2014/09/16)
Provided herein are compounds, compositions and methods for the treatment of Flaviviridae infections, including HCV infections. In certain embodiments, the compounds are according to Formula 2001: where PD, Base, RA and RB are as provided herein. In certain embodiments, compounds and compositions of nucleoside derivatives are disclosed, which can be administered either alone or in combination with other anti-viral agents.
A concise route to L-azidoamino acids: L-azidoalanine, L-azidohomo-alanine and L-azidonorvaline
Roth, Stefanie,Thomas, Neil R.
scheme or table, p. 607 - 609 (2010/09/18)
A simple and highly efficient synthetic route to three homologous azidoamino acids, starting from inexpensive, commercially available, protected natural amino acids is reported. The products can be used to introduce bioorthogonal handles into proteins. Ge
Design and synthesis of potent non-polyglutamatable quinazoline antifolate thymidylate synthase inhibitors
Marsham, Peter R.,Wardleworth, J. Michael,Boyle, F. Thomas,Hennequin, Laurent F.,Kimbell, Rosemary,Brown, Melody,Jackman, Ann L.
, p. 3809 - 3820 (2007/10/03)
The synthesis is described of a series of analogues of the potent thymidylate synthase (TS) inhibitor, N-[4-[N-[(3,4-dihydr0-2,7-dimethyl-4- oxo-6-quinazolinyl)methyl]-N-prop-2-ynylamino]2-fluorobenzoyl]-L-glutamic acid (4, ZM214888), in which the glutami
