Strategies towards the synthesis of anti-tuberculosis drugs

2019 ◽  
Vol 17 (22) ◽  
pp. 5428-5459 ◽  
Author(s):  
Haridas B. Rode ◽  
Dhanaji M. Lade ◽  
René Grée ◽  
Prathama S. Mainkar ◽  
Srivari Chandrasekhar
Keyword(s):  
Asymmetric Synthesis ◽  
Solid Phase Synthesis ◽  
Solid Phase ◽  
Microbial Transformations ◽  
Phase Synthesis

In this report, we reviewed the strategies towards the synthesis of anti-tuberculosis drugs. They include semisynthetic approaches, resolution based strategies, microbial transformations, solid phase synthesis, and asymmetric synthesis.

Asymmetric Synthesis of Cycloalkenyl and Alkenyloxiranes from Allylic Sulfoximines and Aldehydes and Application to Solid-Phase Synthesis.

ChemInform ◽  
2004 ◽  
Vol 35 (31) ◽  
Author(s):  
Hans-Joachim Gais ◽  
Gadamsetti S. Babu ◽  
Markus Guenter ◽  
Parthasarathi Das
Keyword(s):  
Asymmetric Synthesis ◽  
Solid Phase Synthesis ◽  
Solid Phase ◽  
Phase Synthesis

Synthesis and Screening of A DNA-Encoded Library of Non-Peptidic Macrocycles

2020 ◽  
Author(s):  
Eric Koesema ◽  
Animesh Roy ◽  
Nicholas G. Paciaroni ◽  
Thomas Kodadek
Keyword(s):  
Solid Phase Synthesis ◽  
Solid Phase ◽  
Cell Permeability ◽  
Phase Synthesis ◽  
Protein Ligands ◽  
High Affinity ◽  
Scaffold Diversity

There is considerable interest in the development of libraries of non-peptidic macrocycles as a source of ligands for difficult targets. We report here the solid-phase synthesis of a DNA-encoded library of several hundred thousand thioether-linked macrocycles. The library was designed to be highly diverse with respect to backbone scaffold diversity and to minimize the number of amide N-H bonds, which compromise cell permeability. The utility of the library as a source of protein ligands is demonstrated through the isolation of compounds that bind streptavidin, a model target, with high affinity.

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