scholarly journals Combining Flavin Photocatalysis with Parallel Synthesis: A General Platform to Optimize Peptides with Non-Proteinogenic Amino Acids

2021 ◽  
Author(s):  
Jacob Immel ◽  
Maheshwerreddy Chilamari ◽  
Steven Bloom
Keyword(s):  
Amino Acids ◽  
Peptide Synthesis ◽  
Solid Phase ◽  
Solid Phase Peptide Synthesis ◽  
Structure Activity Relationship ◽  
Parallel Synthesis ◽  
Activity Relationship ◽  
Peptide Drugs ◽  
Sar Studies ◽  
Structure Activity

Most peptide drugs contain non-proteinogenic amino acids (NPAAs), born out through extensive structure-activity relationship (SAR) studies using solid-phase peptide synthesis (SPPS). Synthetically laborious and expensive to manufacture, NPAAs also can...

scholarly journals Polymer-Supported Synthesis of Various Pteridinones and Pyrimidodiazepinones

Molecules ◽  
2021 ◽  
Vol 26 (6) ◽  
pp. 1603
Author(s):  
Jan Chasák ◽  
Lucie Brulíková
Keyword(s):  
Building Block ◽  
Solid Phase ◽  
Structure Activity Relationship ◽  
Synthetic Methods ◽  
Activity Relationship ◽  
Synthetic Approach ◽  
Sar Studies ◽  
Structure Activity ◽  
Pharmacokinetic Properties ◽  
Polymer Supported

In this report, we employed the solid-phase synthetic approach to prepare variously substituted dihydropteridinones, tetrahydropyrrolopteridinones, and pyrimidodiazepinones, using a versatile building block-4,6-dichloro-5-nitropyrimidine. All these compounds are pharmacologically significant scaffolds of the great importance of medicinal chemists. The fast and efficient synthetic methodology is highly desirable for defining their structure-activity relationship (SAR) and optimizing pharmacokinetic properties. Our research efforts utilize simple synthetic methods to generate a library of analogues for future SAR studies. The efficiency of our approach was exemplified in various pteridinones as well as pyrimidodiazepinones.

ChemInform Abstract: 4-Methoxybenzyloxycarbonyl Amino Acids in Solid Phase Peptide Synthesis.

ChemInform ◽  
1988 ◽  
Vol 19 (16) ◽  
Author(s):  
S. S. WANG ◽  
S. T. CHEN ◽  
K. T. WANG ◽  
R. B. MERRIFIELD
Keyword(s):  
Amino Acids ◽  
Peptide Synthesis ◽  
Solid Phase ◽  
Solid Phase Peptide Synthesis

scholarly journals Potent α-amino-β-lactam carbamic acid ester as NAAA inhibitors. Synthesis and structure–activity relationship (SAR) studies

2016 ◽  
Vol 111 ◽  
pp. 138-159 ◽  
Author(s):  
Andrea Nuzzi ◽  
Annalisa Fiasella ◽  
Jose Antonio Ortega ◽  
Chiara Pagliuca ◽  
Stefano Ponzano ◽  
...  
Keyword(s):  
Acid Ester ◽  
Structure Activity Relationship ◽  
Activity Relationship ◽  
Carbamic Acid ◽  
Sar Studies ◽  
Structure Activity

On the use of s-t-butylsulphenyl group for protection of cysteine in solid-phase peptide synthesis using fmoc-amino acids

Tetrahedron ◽  
1987 ◽  
Vol 43 (12) ◽  
pp. 2675-2680 ◽  
Author(s):  
Ramon Eritja ◽  
J.Paige Ziehler-Martin ◽  
Peter A. Walker ◽  
Terry D. Lee ◽  
Kassu Legesse ◽  
...  
Keyword(s):  
Amino Acids ◽  
Peptide Synthesis ◽  
Solid Phase ◽  
Solid Phase Peptide Synthesis
Sign in / Sign up

Export Citation Format

Share Document