Synthesis of pyrazine based amidoximes

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Table of contents

Chapter 1: Introduction
1. Introduction
2. Pyridine and pyrazine heterocycles as scaffolds for peptidomimetics
3. Amidoximes and masked amidoximes as prodrugs of amidines, an arginine mimics .
4. Amidoximes as NO donors
Chapter 2: Synthesis of Pyridine and Pyrazine-based Peptidomimetics
1. Introduction
2. Synthetic plan
3. Synthesis of starting 2-cyanonicotinic and 3-cyanopyrazine-2-carboxylic acids
4. Synthesis of peptidomimetics bearing amidoxime function
4.1 Synthesis of amidoximes
4.2 Synthesis of pyridine based amidoximes
4.3 Synthesis of pyrazine based amidoximes
5. Studies towards the synthesis of 1,2,4-oxadiazoles via amidoxime ester units
5.1 Overview of synthetic approaches to 3,5-disubstituted 1,2,4-oxadiazoles via amidoxime esters
5.2 Acylation of amidoximes with further conversion into amino acid derived 1,2,4- oxadiazoles
6. Studies towards the synthesis of 1,2,4-triazoles via N-acylamidrazones
6.1 Overview of synthetic approaches via N-acylamidrazones
6.2 Synthesis of pyridine(pyrazine)-based N-acylamidrazones with further conversion into amino acid derived 1,2,4-triazoles
7. Synthesis of hydrazide modified turn mimics
8. Conclusions
Chapter 3: Structural Analysis
1. Introduction
2. Methods and techniques of conformational study
2.1 Infrared absorption spectroscopy (IR)
2.2 Nuclear Magnetic Resonance spectroscopy (NMR)
2.2.1 One dimensional NMR
2.2.2 Two dimensional NMR
2.3 Molecular modeling
3. Structural and thermodynamic studies of proline-containing peptidomimetics
3.1 Conformational preferences and thermodynamic studies of proline derivatives .
3.2 Stuctural and thermodynamic analysis of pseudotripeptide methyl (2S)-2- ({[(2S)-1-({3-[(Z)-(hydroxyamino)(imino)methyl]pyrazin-2- yl}carbonyl)pyrrolidin-2-yl]carbonyl}amino)-3-phenylpropanoate 7’d
3.2.1 FT-IR and NMR investigations
3.2.2 Molecular modeling
3.2.3 cis-trans isomerization study
3.2.4 A tentative correlation between toxicity and structure
4. Stuctural analysis of esterified amidoximes and oxadiazoles 8, 8’ and 9, 9’
4.1 Conformational analysis of alanine and phenylalanine derivatives 8, 8’ (a,b) and 9, 9’ (a,b)
4.2 Conformational analysis of the proline derivatives 8c, 8’c and 9c, 9’c
5. Structural and thermodynamic studies of acylamidrazones 10, 10’
6. Stuctural analysis of hydrazide modified peptidomimetics 12, 12’
7. Conclusions
Chapter 4: Preliminary Biologycal Evaluation of Amidoximes as NO Donors
General conclusions and perspectives
Chapter 5: Experimental
1. General Methods
2. Experimental procedures
References