Novel Type of Rigid C-Linked Glycosylacetylene−Phenylalanine Building Blocks for Combinatorial Synthesis of C-linked Glycopeptides

1998 ◽  
Vol 63 (26) ◽  
pp. 9657-9668 ◽  
Author(s):  
Todd Lowary ◽  
Morten Meldal ◽  
Arnim Helmboldt ◽  
Andrea Vasella ◽  
Klaus Bock
Keyword(s):  
Building Blocks ◽  
Combinatorial Synthesis

ChemInform Abstract: Novel Type of Rigid C-Linked Glycosylacetylene-Phenylalanine Building Blocks for Combinatorial Synthesis of C-Linked Glycopeptides.

ChemInform ◽  
2010 ◽  
Vol 30 (22) ◽  
pp. no-no
Author(s):  
Todd Lowary ◽  
Morten Meldal ◽  
Arnim Helmboldt ◽  
Andrea Vasella ◽  
Klaus Bock
Keyword(s):  
Building Blocks ◽  
Combinatorial Synthesis

Creating chemical diversity space by scaffold decoration of dihydropyrimidines

2005 ◽  
Vol 77 (1) ◽  
pp. 155-161 ◽  
Author(s):  
Doris Dallinger ◽  
C. Oliver Kappe
Keyword(s):  
Drug Discovery ◽  
Driving Force ◽  
New Technologies ◽  
Materials Science ◽  
Building Blocks ◽  
Chemical Diversity ◽  
Combinatorial Synthesis ◽  
Biologically Active ◽  
Compound Libraries

The demand for diverse compound libraries for screening in drug discovery and materials science is the driving force behind the development of new technologies for rapid parallel and combinatorial synthesis. The focus of this article will be on the scaffold decoration of biologically active dihydropyrimidines (DHPMs) of the Biginelli type, exploring the diversity on all six positions around the scaffold. This opens up the generation of a very large number of analogs given the commercial availability of the building blocks that are used in the functionalization process.

Thiazole and oxazole building blocks for combinatorial synthesis

1999 ◽  
Vol 40 (45) ◽  
pp. 7951-7953 ◽  
Author(s):  
Lenore M. Martin ◽  
Bi-Huang Hu
Keyword(s):  
Building Blocks ◽  
Combinatorial Synthesis

Combinatorial Synthesis of Macrocycles by Multiple Multicomponent Macrocyclization Including Bifunctional Building Blocks (MiB)

Synlett ◽  
2007 ◽  
Vol 2007 (2) ◽  
pp. 0308-0312 ◽  
Author(s):  
Ludger Wessjohann ◽  
Daniel Rivera ◽  
Otilie Vercillo
Keyword(s):  
Building Blocks ◽  
Combinatorial Synthesis

Glycosamino Acids:  New Building Blocks for Combinatorial Synthesis

1996 ◽  
Vol 118 (16) ◽  
pp. 3818-3828 ◽  
Author(s):  
Jason P. McDevitt ◽  
Peter T. Lansbury
Keyword(s):  
Building Blocks ◽  
Combinatorial Synthesis

Cycloelimination-assisted Combinatorial Synthesis of Diverse Heterocyclic Scaffolds of Chemotherapeutic Values

2019 ◽  
Vol 23 (7) ◽  
pp. 768-808
Author(s):  
Virendra Prasad ◽  
Nidhi Mishra ◽  
Anand K. Agrahari ◽  
Sumit K. Singh ◽  
Prabhu P. Mohapatra ◽  
...  
Keyword(s):  
High Throughput ◽  
High Throughput Screening ◽  
Solid Phase ◽  
Combinatorial Libraries ◽  
Building Blocks ◽  
Biological Evaluation ◽  
Molecular Structures ◽  
Combinatorial Synthesis ◽  
Drug Discovery And Development ◽  
Great Ease

Recent advances in high-throughput, automated techniques combined with the identification of new therapeutic targets in genome sequencing and molecular biology have generated a need for a large collection of diverse heterocyclic scaffolds. This inspires toward the development of novel reaction sequences and linking strategies to generate libraries of diverse simple to complex heterocyclic systems. In this regard, combinatorial chemistry has emerged as an excellent technology platform for the rapid assembly of building blocks to synthesize complex molecular structures with great ease in a few synthetic steps. By means of the implementation of high-throughput screening for the biological evaluation of hits and leads, combinatorial libraries have become important assets in drug discovery and development. In the last two decades, the cyclorelease strategy that minimizes the chemical and tethering implications by releasing the intact desired target molecule in the final step of reaction has attracted much attention. Recently, a particular interest is developing in linking strategies, where loading and cleavage steps contribute to the complexity of the target structure rather than only extraneous manipulations. This review summarises the practical and high-yielding approaches of solid phase combinatorial synthesis for diverse high-purity heterocyclic skeletons of pharmacological importance involving the cycloelimination strategy.

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