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N-Sulfonated-N-Heterocycles

Synthesis, Chemistry, and Biological Applications

1st Edition - August 26, 2022

Authors: Galal H. Elgemeie, Rasha A. Azzam, Wafaa A. Zaghary, Ashraf A. Aly, Nadia H Metwally, Mona O. Sarhan, Elshimaa M. Abdelhafez, Rasha E. Elsayed

Paperback ISBN:

9 7 8 - 0 - 1 2 - 8 2 2 1 7 9 - 2

eBook ISBN:

9 7 8 - 0 - 1 2 - 8 2 2 1 8 2 - 2

N-Sulfonated-N-Heterocycles covers the synthesis, chemistry and biological applications of these compounds, focusing on pioneering synthetic approaches, mechanistic insights and… Read more

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N-Sulfonated-N-Heterocycles covers the synthesis, chemistry and biological applications of these compounds, focusing on pioneering synthetic approaches, mechanistic insights and their limitations, as well as recent advances in this field. The synthesis of some of N-sulfonated N-heterocycles and their transformation to other useful cyclic and acyclic compounds are discussed, as well as their uses as useful intermediates in the preparation of polymeric and medicinal materials. This book includes detailed methods and protocols, and the focus on applications makes this resource an essential guide for all researchers in the area of organic, medicinal and polymeric synthetic study.

Cover image
Title page
Table of Contents
Copyright
About the authors
Chapter 1. Synthesis of N-sulfonated aziridines
Abstract
1.1 Introduction
1.2 Synthesis of N-sulfonated aziridines via transferring of nitrogen to alkenes
1.3 Synthesis of N-sulfonated aziridines via transferring of carbon to N-sulfonyl imines
1.4 Synthesis of N-sulfonated aziridines via intramolecular cyclization of amine derivatives
References
Chapter 2. Chemistry of N-sulfonated aziridines and their use in polymerization reactions
Abstract
2.1 Introduction
2.2 Chemistry of N-sulfonated aziridines
2.3 Uses of N-sulfonated aziridines in living aza-anionic polymerization
References
Chapter 3. Synthesis of N-sulfonated azetidines and β-lactemes and their applications
Abstract
3.1 Introduction
3.2 Synthesis of sulfonyl-activated azetidines and azetidin-2-ones
3.3 Chemistry of sulfonyl-activated azetidine and azetidin-2-ones
3.4 Sulfonyl-activated azetidine and azetidin-2-ones in polymerization application
References
Chapter 4. N-Sulfonated N-azoles: Synthesis, chemistry and biological applications
Abstract
4.1 Introduction
4.2 N-Sulfonated pyrroles
4.3 Synthesis of N-tosyl isoxazoles and their derivatives
4.4 Synthesis of N-tosyl oxazoles and their derivatives
4.5 Synthesis of N-tosyl-1,2-thiazole and its derivatives
4.6 Synthesis of N-tosyl thiazole and its derivatives
References
Chapter 5. Synthesis of N-sulfonated N-diazoles, their chemistry and biological assessments
Abstract
5.1 Introduction
5.2 Synthesis of N-sulfonylimidazole and its derivatives
5.3 Uses of N-sulfonylimidazole derivatives
5.4 Chemistry of N-sulfonylpyrazoles
5.5 Chemistry of N-sulfonylthiadiazole derivatives
5.6 Synthesis of 1,3,4-thiadiazole and 1,2,3-thiadiazole derivatives
5.7 Chemistry of N-sulfonyl-1,3,4-oxadiazoles
References
Chapter 6. Synthesis, chemistry and uses of N-sulfonated N-triazoles and N-tetrazoles
Abstract
6.1 Introduction
6.2 Synthesis of N-sulfonyl-1,2,3-triazoles
6.3 Reactions of N-sulfonyl-1,2,3-triazoles
6.4 Chemistry of 1,2,4-triazoles
6.5 Biological activity of some N-sulfonyltriazoles
6.6 Chemistry of N-sulfonyl-1,2,3,4-tetrazoles
References
Chapter 7. Synthetic approaches and biological evaluation of N-sulfonated N-azines
Abstract
7.1 Introduction
7.2 Synthesis of N-sulfonyl pyridinone derivatives and their biological activities
7.3 Synthesis of N-sulfonyl pyridine derivatives and their biological activities
7.4 Synthesis of N-sulfonyl oxazine derivatives and their biological activities
7.5 Synthesis of N-sulfonyl thiazine derivatives
References
Chapter 8. Synthesis of N-sulfonated N-diazines, N-triazines and N-tetrazines; their uses and biological applications
Abstract
8.1 Introduction
8.2 N-Sulfonyldiazines
8.3 N-Sulfonyl-triazines
8.4 N-Sulfonated tetrazines
References
Chapter 9. Synthesis of N-sulfonated N-azepines
Abstract
9.1 Introduction
9.2 N-Sulfonyl azepines
9.3 N-Sulfonyl dihydroazepines
9.4 N-Sulfonyl tetrahydroazepines
References
Chapter 10. Synthesis of N-sulfonated N-benzoazoles and their use in medicinal chemistry
Abstract
10.1 Introduction
10.2 Chemistry of N-sulfonyl indoles
10.3 Synthesis of N-sulfonyl benzoxazole
10.4 Synthesis of N-sulfonyl benzothiazoles
References
Chapter 11. N-Sulfonated N-benzodiazoles and N-benzotriazoles: Synthesis and medicinal activity
Abstract
11.1 Introduction
11.2 N-Sulfonyl benzimidazole
11.3 N-Sulfonyl indazoles
11.4 N-Sulfonyl triazoles
References
Chapter 12. N-Sulfonated N-benzoazines: Synthesis and medicinal chemistry
Abstract
12.1 Introduction
12.2 N-Sulfonyl-cinnolines
12.3 N-Sulfonyl-phthalazine
12.4 N-Sulfonyl-quinazolines
12.5 N-Sulfonyl-quinolines, – isoquinolines and their derivatives
12.6 N-Sulfonyl-quinolinones
12.7 N-Sulfonyl quinoxaline
References
Chapter 13. Patents and applications of N-sulfonated N-heterocycles
Abstract
13.1 Introduction
13.2 Three membered N-sulfonyl heterocycles
13.3 Four-membered N-sulfonyl heterocycles
13.4 Five membered N-sulfonyl heterocycles
13.5 Six membered N-sulfonyl heterocycles
13.6 Fused N-sulfonyl heterocycles
References
Index

Galal H. Elgemeie

Galal H. Elgemeie is the author of over 270 scientific international papers on heterocyclic chemistry and medicinal chemistry. His research interests include the development and mechanistic understanding of organic reactions and their application to the synthesis of antimetabolic agents. He was an international elected member of the Scientific Board of the International Basic Sciences Programme (IBSP), UNESCO, in Paris, France. He was a postdoctoral fellow of the Alexander von Humboldt Foundation in Germany, the Fulbright in USA, the British Council in England, and then the German Research Foundation (DFG) in Germany. He supervised several cooperation projects with the European Community under the TEMUPS programme, Prof. Elgemeie was nominated as one of the leading scientists of the COMSTECH in the year 2009 Report. Prof. Elgemeie's research activities have received many awards including The African Union Scientific Award "Continental Scientific Award" in Science and Technology, The ISESCO Scientific Award and The Egypt State Honor Award "NILE", among many others.

Affiliations and expertise

Department of Chemistry, Helwan University, Cairo, Egypt

Rasha A. Azzam

Rasha Azzam, Professor of Organic Chemistry, is an active researcher in the area of organic chemistry (from drug design and synthesis to drug delivery). She obtained her PhD from Catholic University of Leuven, Belgium, under a research fellowship and supervision of Distinguished Research Prof. Georges Hoornaert and Prof. Frans Compernolle. After her PhD, she assumed her position as an Assistance Professor at Helwan University. During her tenure at Helwan University, she was appointed as assistant/associate professor at three different universities before returning back to her position at Helwan University. Azzam was awarded the Outstanding Faculty Member Award in 2007 and the Silver Medal from ASRT in 2018. She has published more than forty international peer-reviewed publications in addition to several international conference presentations. She has supervised more that fifteen graduate-level theses and secured funding for over seven major educational grants.

Affiliations and expertise

Professor of Organic Chemistry, Chemistry Department, Faculty of Science, Helwan University, Cairo, Egypt

Wafaa A. Zaghary

Wafaa Zaghary is a Professor of Pharmaceutical Chemistry, the head and founder of Pharmaceutical Chemistry Department, Faculty of Pharmacy, Helwan University. She is one of the expert Egyptian medicinal chemists especially in the design and synthesis of new chemical scaffolds targeting cancer. In addition, she had been involved in the nano-nuclear pharmacy research and radiopharmaceutical fields. Prof. Zaghary with her group had discovered novel tumor imaging agent with nanographene oxide sheets (2022), DNA gyrase & topoisomerase IV inhibitors (2021), Novel thienopyrimidine analogues as potent mGR-1 inhibitors with anticancer activity (2021), coumarin-based lead compound with CDK-4 inhibitory and anticancer activity (2021), Nano-selenium platforms as protective agents for hepatocellular carcinoma (2021), new aldose reductase inhibitors with anticancer action (2019), potential EGFR inhibitors (indazole, quinazoline, and quinolones) (2019). She has been involved in many research projects (Helwan University), (King Saud University) and (National Research Centre in Egypt). In 2018, She received the ‘’outstanding research award’’ Helwan University.

Affiliations and expertise

Professor of pharmaceutical chemistry at Pharmaceutical Chemistry Department, Faculty of Pharmacy, Helwan University, Helwan, Cairo, Egypt

Ashraf A. Aly

Prof Ashraf Aly, is Professor of Organic Chemistry, Chemistry Department, Faculty of Science, Minia University, El-Minia, Egypt. He Work as a Vice Dean for Community Service and Environmental Development. He published nearly 180 papers (H-index: 24). He got the State’s Encouragement National Prize in Organic Chemistry (2004), and the University Appreciation Prize in Basic Sciences (2019). International University Publication prizes from 2013 till 2021. He got scholarships: DFG, DAAD and 3-MET. He is an Editorial board and a reviewer, in numerous international journals and a membership in the permanent committee for the promotion degree for Professors. He was in the scientific group of Prof Henning Hopf, Institute of Organic Chemistry, Braunschweig University, Germany. He has a prospective collaboration with Prof Stefan Bräse, Karlsruhe Institute of Technology, Germany and Prof Alan B. Brown, Florida Institute of Technology, USA.

Affiliations and expertise

Professor of organic chemistry at Chemistry Department, Faculty of Science, Minia University, El-Minia, Egypt

Nadia H Metwally

Prof. Nadia Metwally, is Professor of Organic Chemistry in Faculty of Science, Cairo University. Her research interests include the synthesis of N-sulfonated heterocyclic compounds and their applications, green chemistry and medicinal chemistry. She supervised the work of more than 35 master and doctoral students in synthesis of heterocyclic compounds as anticancer, antiviral, antimicrobial and drug delivery. She is a referee for several International and National scientific Journals. She has published more than 75 papers in different journals related to Elsevier and Springer, Bentham and others. Prof. Metwally research activities have received many awards including the Cairo University prize for the distinct researches in Chemistry in 2007. Prof. Nadia Metwally supervised several cooperation projects such as a project with Egyptian Academy of Scientific Research and Technology entitled Design and synthesis of some novel N-sulfonylated pyrazoles as inhibitors of coronavirus.

Affiliations and expertise

Professor of organic chemistry at Chemistry Department, Faculty of Science, Cairo University, Giza, Egypt

Mona O. Sarhan

Mona Sarhan is the lecturer of Radiopharmaceutical Chemistry at the Egyptian Atomic Energy Authority and an IAEA trained Radio-pharmacist. A member of the quality control team in the Egyptian-Chinese project for production of Gel 99m-Technitium generators. Since 2018 she has been a visiting lecturer at different Egyptian Universities teaching medicinal chemistry and the basic concepts of drug design. Currently, her research interest links the fields of medicinal chemistry, organic chemistry, rational design and radio-pharmacy to seek an opportunity to develop targeted therapeutics.

Affiliations and expertise

Associate Professor of pharmaceutical chemistry at Pharmaceutical Chemistry Department, Egyptian Atomic Energy Authority, Cairo, Egypt

Elshimaa M. Abdelhafez

Elshimaa Abdelhafez, is Associate professor of Medicinal Chemistry, Faculty of Pharmacy, Minia University, Minia, Egypt. In 2008, she received her master degree from Faculty of Pharmacy, Minia University, meanwhile, in 2013; her PhD was in pharmaceutical medicinal chemistry as a channel scholarship between wake forest university, North Carolina, USA and Minia University, Minia, Egypt. She has earned six national awards for publication from Minia University for the period 2016 to 2021. She published 28 literatures in various international journals and 7 national papers. She writes and develops educational materials and contributes in teaching special topics in organic synthesis and medicinal chemistry for 18 years.

Affiliations and expertise

Associate Professor of Medicinal chemistry at Medicinal Chemistry Department, Faculty of Pharmacy, Minia University, El-Minia, Egypt

Rasha E. Elsayed

Rasha Essam, a senior research assistant at American University in Cairo (AUC), obtained her MSc degree in organic chemistry from Helwan University in 2019 under the supervision of Professor Galal Elgemeie. Her master research focused on preparation of biologically active sulfonamide analogs and loading the most potent antibacterial compounds into nanofiber delivery systems for their use in wound healing. In 2017 till now, she worked as research assistant in two scientific projects at the laboratory of Professor Tarek Madkour, at AUC, where she developed biodegradable polymer composites, in addition to functionalization of natural polymers. One of these projects is awarded the Silver Medal from Academy of Scientific Research and Technology in 2018.

Affiliations and expertise

Researcher, Chemistry Department, Faculty of Science, Helwan University, Helwan, Cairo, Egypt