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Carbon-carbon and carbon-heteroatom bond-forming reactions are the backbone of synthetic organic chemistry. Scientists are constantly developing and improving these techniques in order to maximize the diversity of synthetically available molecules. These techniques must be developed in a sustainable manner in order to limit their environmental impact. This book highlights green bond forming reactions for bioactive scaffolds.
This book addresses the various classes of privileged scaffolds and covers the history of their discovery and use.
A major challenge to finding compounds that modulate protein function is the identification of chemical matter for screening. Although Nature provides excellent options for screening in the form of natural products, sufficient quantities can be difficult to obtain and characterize. Thus, chemical synthesis plays a lead role in providing molecules for screening, and chemists must ultimately decide what to synthesize based on the predicted value of the end products. We developed new synthetic strategies to access compounds for screening. In each case, natural products serve as an inspiration for the developed chemistry. First, a strategy was developed that provides access to scaffolds based on bioactive alkaloids and terpenoids. A key feature of this strategy is the use of transition metals to mediate the synthesis of multiple scaffolds from simple enynes and diynes. A t -butylsulfinamide group serves as a convenient tether to facilitate this chemistry. Principal component analysis (PCA) is used to analyze the relationship of our synthetic scaffolds to naturally occurring alkaloids and terpenoids. Then, a chemical reaction was studied that provides access to benzannulated medium rings inspired by natural products. In the developed reaction, three reagent classes (TsOH, Cu[BF 4 ] 2 , and Tf 2 0) were shown to polarize the carbonyl of a polycyclic cyclohexadienone and subsequently cause a cationic fragmentation reaction that generates an aromatic ring annulated to a medium ring. This process efficiently produces 7- to 11- membered rings while tolerating a variety of common functional groups. Work is presented on efforts to apply this reaction to the synthesis of two natural products, heliannuol A and puerol A.
Bioactive Glasses: Materials, Properties and Applications, Second Edition provides revised, expanded and updated content on the current status of this unique material, including its properties, technologies and applications. The book is suitable for those active in the biomaterials and bioengineering field, and includes eight new chapters that cover material types, computational modeling, coatings and applications. Chapters deal with the materials and mechanical properties of bioactive glass and the applications of bioactive glasses, covering their uses in wound healing, maxillofacial surgery and bone tissue engineering, among other topics. With its distinguished editor and expert team of international contributors, the book is an invaluable reference for researchers and scientists in the field of biomaterials, both in academia and industry. Provides a detailed review of bioactive glasses, their properties, technologies and applications Comprehensively covers the materials and mechanical properties of bioactive glass and their further applications, including wound healing, maxillofacial surgery and bone tissue engineering Suitable for those active in the biomaterials and bioengineering field
Discover an enhanced synthetic approach to developing and screening chemical compound libraries Diversity-oriented synthesis is a new paradigm for developing large collections of structurally diverse small molecules as probes to investigate biological pathways. This book presents the most effective methods in diversity-oriented synthesis for creating small molecule collections. It offers tested and proven strategies for developing diversity-oriented synthetic libraries and screening methods for identifying ligands. Lastly, it explores some promising new applications based on diversity-oriented synthesis that have the potential to dramatically advance studies in drug discovery and chemical biology. Diversity-Oriented Synthesis begins with an introductory chapter that explores the basics, including a discussion of the relationship between diversity-oriented synthesis and classic combinatorial chemistry. Divided into four parts, the book: Offers key chemical methods for the generation of small molecules using diversity-oriented principles, including peptidomimetics and macrocycles Expands on the concept of diversity-oriented synthesis by describing chemical libraries Provides modern approaches to screening diversity-oriented synthetic libraries, including high-throughput and high-content screening, small molecule microarrays, and smart screening assays Presents the applications of diversity-oriented synthetic libraries and small molecules in drug discovery and chemical biology, reporting the results of key studies and forecasting the role of diversity-oriented synthesis in future biomedical research This book has been written and edited by leading international experts in organic synthesis and its applications. Their contributions are based on a thorough review of the current literature as well as their own firsthand experience developing synthetic methods and applications. Clearly written and extensively referenced, Diversity-Oriented Synthesis introduces novices to this highly promising field of research and serves as a springboard for experts to advance their own research studies and develop new applications.
The presented research work comprises of synthesis, spectral analysis and biological screening of some new acetamides/sulfides bearing substituted-1,3,4-Oxadiazole and morpholine moieties. The acetamide, 1,3,4-oxadiazole and morpholine moieties are important functionalities because of their broad range of known pharmacological activities. Synthetic approaches were utilized to synthesize poly-functional compounds. The main intention of the present research work was to design and synthesize some new poly-functional compounds having 1,3,4-oxadiazole and acetamide or 1,3,4-oxadiazole, morpholine and sulfide or 1,3,4-oxadiazole, morpholine and acetamide moieties together in one molecule. It was assumed that 2,5-disubstituted-1,3,4-oxadiazol ring along with the potential morpholine moiety and acetamide/sulfide functionality will enhance the activity of the molecule. Keeping in sight the broad diversity of biological activitites, some of the synthesized compounds were checked for their antibacaterial, hemolytic and antifungal screening. Some of compounds were found to be active and showed interesting results as compared to reference standard drugs.