Parallel Solid-Phase Synthesis and High-Throughput1H NMR Evaluation of a 96-Member 1,2,4-Trisubstituted-pyrimidin-6-one-5-carboxylic Acid Library

2009 ◽  
Vol 11 (3) ◽  
pp. 469-480 ◽  
Author(s):  
Bruce C. Hamper ◽  
Allen S. Kesselring ◽  
Robert C. Chott ◽  
Shengtian Yang
Keyword(s):  
Carboxylic Acid ◽  
Solid Phase Synthesis ◽  
Solid Phase ◽  
Phase Synthesis

Synthesis and biological properties of vasopressin analogues containing 1,2,3,4-tetrahydroisoquinoline-3-carboxylic acid

1990 ◽  
Vol 55 (4) ◽  
pp. 1099-1105 ◽  
Author(s):  
Zdenko Procházka ◽  
Juris E. Ancans ◽  
Jiřina Slaninová ◽  
Alena Machová ◽  
Tomislav Barth ◽  
...  
Keyword(s):  
Amino Acid ◽  
Carboxylic Acid ◽  
Solid Phase Synthesis ◽  
Solid Phase ◽  
Biological Activities ◽  
Biological Properties ◽  
Phase Synthesis ◽  
Aromatic Residues ◽  
Synthesis Methodology ◽  
Vasopressin Analogues

Solid phase synthesis methodology on a benzhydrylamine resin was used for the synthesis of three analogues of vasopressin with the non-coded amino acid, 1,2,3,4-tetrahydroisoquinoline-3-carboxylic acid (Tic), in the position 2 ([Tic2, Lys8]VP (I)) and in the position 3 ([Tic3, Lys8]VP (II)). The analogue containing only one Tic in place of both aromatic residues was also isolated (des-Tyr2-[Tic3, Lys8]VP (III)). The biological activities of all analogues were negligible.

Strategies for the Synthesis of Hydroxamic Acids

2018 ◽  
Vol 15 (2) ◽  
pp. 154-165 ◽  
Author(s):  
Ankit Ganeshpurkar ◽  
Devendra Kumar ◽  
Sushil K. Singh
Keyword(s):  
Cardiovascular Diseases ◽  
Carboxylic Acid ◽  
Organic Compounds ◽  
Acid Chloride ◽  
Solid Phase Synthesis ◽  
Solid Phase ◽  
Allergic Diseases ◽  
Hydroxamic Acids ◽  
Phase Synthesis ◽  
Major Class

Background: Hydroxamic acids are a major class of organic compounds. They have a wide variety of pharmacological actions in targeting cancers, cardiovascular diseases, HIV, Alzheimer's disease, Malaria, Allergic diseases. Objective: The present review focuses on the chemistry of conventional and non-conventional routes for the synthesis of hydroxamic acids reported till date. Conclusion: The hydroxamic acids are conventionally synthesized via carboxylic acid and their acid chloride derivatives. However, some other functional groups i.e. aldehyde, amine, amide and alcohol can also be converted to hydroxamate with ease. The solid phase synthesis techniques are also gaining importance for the synthesis of hydroxamic acids and these pathways have opened a wide arena for the synthesis of diverse and complex hydroxamic acids.

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