Alpha-glucosidase inhibitors : clinically promising candidates for anti-diabetic drug discovery

__Alpha-glucosidase Inhibitors: Clinically Promising Candidates for Anti-diabetic Drug Discovery__ presents information that researchers can use to address a whole host of promising leads for the development of novel, oral, anti-diabetic drugs with improved efficacy and fewer side effects. Beginning with a discussion of the huge potential of a -glucosidase inhibitor leads and adaptations, and highlighting their importance within the field of anti-diabetic drug discovery, the book provides chemical structures, detailed background information and __in vivo__ and __in vitro__ biological activity data, and more economical adaptations of these structures. Drawing on the author's expert research in the field, this book highlights promising leads for development and helps researchers select the most appropriate inhibitors for their own work. It is a useful tool not only for anti-diabetic drug development researchers, but also for those whose research may be enhanced by an understanding of a -glucosidase inhibitor chemistry and activity. Alpha-Glucosidase Inhibitors Copyright Quote from the Quran Dedication Contents About the author Preface Acknowledgments one Introduction, rationale and the current clinical status of oral α-glucosidase inhibitors 1.1 Introduction 1.2 Diabetes mellitus and the antidiabetic drugs 1.3 α-Glucosidase inhibitors—past and present 1.4 Rationale References two Natural and synthetic sugar mimics 2.1 Introduction 2.2 Iminosugars 2.2.1 Polyhydroxylated pyrrolidines 2.2.2 Polyhydroxylated pyrrolizidines 2.2.3 Polyhydroxylated quinolizidines 2.2.4 Hydroxymethyl-branched polyhydroxylated indolizidines 2.2.5 Nojirimycin derivatives 2.2.6 Other derivatives 2.3 Aminosugars 2.4 Thiosugars 2.5 Carbasugars References three Polyphenols 3.1 Chalcones 3.2 Xanthones 3.3 Flavonoids and other polyphenols References four Terpenoids and steroids 4.1 Terpenoids 4.2 Steroid derivatives References five Azoles and related derivatives 5.1 Thiadiazoles, oxadiazoles, and triazoles 5.2 Other related derivatives 5.2.1 Oxindoles 5.2.2 2-Arylquinazolin-4(3H)-one derivatives 5.2.3 Bis-Indolylmethanes 5.2.4 Metallophthalocyanines 5.2.5 Thiobarbiturates 5.2.6 Carbazoles and hydrazone-bridged thiazole-pyrrole derivatives References six Cyclitols and miscellaneous inhibitors 6.1 Cyclitols 6.2 Polycyclitols 6.3 Aminocyclitols 6.4 Conduritols 6.5 Inositols 6.6 Miscellaneous derivatives 6.6.1 Anthraquinones 6.6.2 Sarcoviolins and terphenyl derivatives 6.6.3 Stilbenes 6.6.4 Stilbene-based urea derivatives 6.6.5 Depsidones 6.6.6 Macrolides 6.6.7 Peptides 6.6.8 Ganomycin I and its derivatives 6.6.9 Carbenes 6.6.10 Pyranoquinolinyl-acrylic acid diastereomers 6.6.11 N,N′-bis-Cyanomethylamine and alkoxymethylamine derivatives References seven Computational and structural biology of α-glucosidase-inhibitor complexes: clues to drug optimization and development 7.1 Crystal structure of human MGAM-C in complex with acarbose 7.2 Crystal structures of human MGAM-N in complex with acarbose, miglitol, and salacinol 7.3 Comparison of the MGAM-N-inhibitor complexes 7.4 The human MGAM-N-salacinol derivative complexes 7.5 Comparison of the crystal structures of acarbose in complex with MGAM-C, MGAM-N, and SI-N 7.6 Important structural and functional clues to human MGAM-N inhibition 7.7 The human MAGAM-N-casuarine complex 7.8 Crystal structures of free isomaltase and in complex with maltose 7.9 Insights into the α-glucosidase mechanism of inhibition 7.10 Computational simulations of α-glucosidase-inhibitor interactions 7.10.1 The 3′-benzylated analog of 3′-epi-neoponkoranol 7.10.2 Fluorescent DNJ derivatives 7.10.3 The 5-arylidene-N,N-diethylthiobarbiturate derivatives 7.10.4 The 3′-O-neopentyl derivative of salacinol 7.10.5 Salvianolic acids C and A 7.10.6 Pelargonidin-3-o-rutinoside and analogs 7.10.7 Sericin peptide References Appendix A comprehensive list of promising α-glucosidase inhibitors with the activity data discussed in the book Index Alpha-glucosidase Inhibitors: Clinically Promising Candidates for Anti-diabetic Drug Discovery presents information that researchers can use to address a whole host of promising leads for the development of novel, oral, anti-diabetic drugs with improved efficacy and fewer side effects. Beginning with a discussion of the huge potential of α -glucosidase inhibitor leads and adaptations, and highlighting their importance within the field of anti-diabetic drug discovery, the book provides chemical structures, detailed background information and in vivo and in vitro biological activity data, and more economical adaptations of these structures. Drawing on the author’s expert research in the field, this book highlights promising leads for development and helps researchers select the most appropriate inhibitors for their own work. It is a useful tool not only for anti-diabetic drug development researchers, but also for those whose research may be enhanced by an understanding of α -glucosidase inhibitor chemistry and activity.