Expedient Method for the Solid-Phase Synthesis of Aspartic Acid Protease Inhibitors Directed toward the Generation of Libraries

1995 ◽  
Vol 38 (9) ◽  
pp. 1427-1430 ◽  
Author(s):  
Ellen K. Kick ◽  
Jonathan A. Ellman
Keyword(s):  
Protease Inhibitors ◽  
Aspartic Acid ◽  
Solid Phase Synthesis ◽  
Solid Phase ◽  
Acid Protease ◽  
Phase Synthesis

Solid-phase synthesis of potential aspartic acid protease inhibitors containing a hydroxyethylamine isostere

1999 ◽  
Vol 40 (14) ◽  
pp. 2729-2732 ◽  
Author(s):  
Jinglan Zhou ◽  
Andreas Termin ◽  
Melissa Wayland ◽  
Christine M. Tarby
Keyword(s):  
Protease Inhibitors ◽  
Aspartic Acid ◽  
Solid Phase Synthesis ◽  
Solid Phase ◽  
Acid Protease ◽  
Phase Synthesis

Solid Phase Synthesis of Novel Fullerene Nucleotides Conjugates

2011 ◽  
Vol 266 ◽  
pp. 200-203
Author(s):  
Jing Zhang ◽  
Ya Dong Zhang
Keyword(s):  
Aspartic Acid ◽  
Solid Phase Synthesis ◽  
Solid Phase ◽  
Biological Properties ◽  
Azomethine Ylide ◽  
Hydroxyl Group ◽  
Spectrometric Analysis ◽  
Phase Synthesis ◽  
Chemical Structures ◽  
Controlled Pore Glass

N-substituted 3, 4-fullero pyrrolidine was synthesized according to 1, 3-dipolar cycloaddition of the azomethine ylide. Aspartic acid with protected α-amino and α-carboxyl groups was reacted with the activated hydroxyl group of N-substituted 3, 4-fullero pyrrolidine. The products were deprotected, affording the monofullerene aspartic acid (mFas). The conjugate FasT was synthesized by reaction of mFas containing protected amino group with the thymidylic acid derivatived controlled pore glass (CPG) using solid phase synthesis. All of the above fullerene derivatives were characterized by UV–vis, 1H NMR, IR and MS spectrometric analysis, giving the correct spectra with regard to their chemical structure. The chemical structures of fullerene nucleotides conjugate FasT is different from previous reports and may have novel biological properties. Moreover, they are more suitable for applications in biomedical research due to their solubilization in THF and DMSO. They have a potential to be used as monomer for the automatic synthesis. It allows further conjugation with specific biomolecules including amino acids, peptides, nucleotides and nucleic acids. A novel method has been developed to synthesize fullerene nucleotides conjugate. Their unique chemical structures make them very interesting for their potential use in medicine and biology.

Solid-phase synthesis of benzisothiazolones as serine protease inhibitors

1999 ◽  
Vol 9 (5) ◽  
pp. 663-666 ◽  
Author(s):  
Kuo-Long Yu ◽  
Rita Civiello ◽  
Daniel G.M. Roberts ◽  
Steven M. Seiler ◽  
Nicholas A. Meanwell
Keyword(s):  
Serine Protease ◽  
Protease Inhibitors ◽  
Solid Phase Synthesis ◽  
Solid Phase ◽  
Serine Protease Inhibitors ◽  
Phase Synthesis

Solid-phase synthesis of tailed cyclic peptides: The use of α-allyl-protected aspartic acid leads to aspartimide and tetramethylguanidinium formation

1996 ◽  
Vol 3 (2) ◽  
pp. 89-97 ◽  
Author(s):  
Dominique Delforge ◽  
Marc Dieu ◽  
Edouard Delaive ◽  
Muriel Art ◽  
Barbara Gillon ◽  
...  
Keyword(s):  
Aspartic Acid ◽  
Cyclic Peptides ◽  
Solid Phase Synthesis ◽  
Solid Phase ◽  
Phase Synthesis

Solid-phase synthesis of a library based on biphenyl-containing trypsin-like serine protease inhibitors

2009 ◽  
Vol 19 (22) ◽  
pp. 6477-6480 ◽  
Author(s):  
Shuhao Shi ◽  
Shirong Zhu ◽  
Samuel W. Gerritz ◽  
Bogumila Rachwal ◽  
Zheming Ruan ◽  
...  
Keyword(s):  
Serine Protease ◽  
Protease Inhibitors ◽  
Solid Phase Synthesis ◽  
Solid Phase ◽  
Serine Protease Inhibitors ◽  
Phase Synthesis
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