Meet the editor

Maria Marinescu received her PhD in 2010 from the University of Bucharest, under the supervision of Prof. Mihaela Hillebrand, studying the chemistry and the electronic structure of the 1,2,3,4,5,6,7,8-octahydroacridine compounds, as key structures for new biomolecules and hydrogen-bonding receptors. Dr. Marinescu is currently an assistant professor at the University of Bucharest, Department of Organic Chemistry, Biochemistry and

Catalysis. Her current research interests are in organic synthesis of various heterocycles with applications in medicinal and materials chemistry, density functional theory studies in organic molecules related with their biological properties, and applications of organic materials in art and archaeology.

Contents

**Section 1**

**Section 2**

Benzimidazole and Its Derivatives

*by Jørn H. Hansen and Richard Fjellaksel*

*by Maria Marinescu*

*and Sivaraman Rosepriya*

*by Kantharaju Kamanna*

*and Olga N. Zhukovskaya*

*and Vincent C.O. Njar*

**Section 3**

**Preface III**

Introduction to Chemistry and Applications of Benzimidazoles **1**

**Chapter 1 3**

Chemistry of Benzimidazoles **13**

**Chapter 2 15**

**Chapter 3 31**

**Chapter 4 51**

The Therapeutic Potential of Benzimidazoles **71**

**Chapter 5 73**

**Chapter 6 89**

X-Ray Crystal Structure Analysis of Selected Benzimidazole Derivatives *by Aravazhi Amalan Thiruvalluvar, Gopalsamy Vasuki, Jayaraman Jayabharathi* 

Introductory Chapter: Short Insight in Synthesis and Applications of

Catalytic Intermolecular Functionalization of Benzimidazoles

Synthesis and Pharmacological Profile of Benzimidazoles

*by Alexander A. Spasov, Pavel M. Vassiliev, Vera A. Anisimova* 

Development of Benzimidazole Compounds for Cancer Therapy *by Puranik Purushottamachar, Senthilmurugan Ramalingam* 

Antidiabetogenic Features of Benzimidazoles

## Contents



Preface

Finding new strategies for synthesizing benzimidazole derivatives and functionalizing the benzimidazole core has proved to be important due to the compound's various applications in medicine, chemistry, and other areas. The development of new domains, such as the chemistry of optically active benzimidazole compounds, is imperative because of the compounds' particular pharmacological properties and

The multitude of benzimidazole derivatives marketed as drugs has led to intensive research in the field for the discovery of new biologically active structures. The general applications of benzimidazole derivatives in materials chemistry, electronics, technology, dyes, pigments, and agriculture open up new research horizons. This book guides the rational design of benzimidazole derivatives synthesis with certain

Section I: **Introduction to Chemistry and Applications of Benzimidazoles**

Chapter 2 "**Catalytic Intermolecular Functionalization of Benzimidazoles**" presents an updated review on functionalizations of nitrogen and at position C–2 in the benzimidazole scaffold. Functionalization of positions C–4 through C–7 is more challenging as these are less activated. A key success factor for reactions is the

Chapter 3 "**X-Ray Crystal Structure Analysis of Selected Benzimidazole Derivatives**" describes the X-ray crystal structure analysis of six selected benzimidazole derivatives. The detailed structural analyses indicate that the planes of benzimidazole units are associated in different modes through hydrogen bonds.

Chapter 4 "**Synthesis and Pharmacological Profile of Benzimidazoles**" summarizes the synthetic methods of benzimidazole derivatives and discusses therapeutic use of benzimidazole in conditions like diabetes, cancer, parasitic diseases, viruses,

Chapter 5 "**Antidiabetogenic Features of Benzimidazoles**" examines the effect of a new cyclic aminobenzimidazole derivative, diabenol, which contains a guanidine group and combines pharmacological effects of biguanides and sulfonylurea deriva-

Chapter 1 "**Introductory Chapter: Short Insight in Synthesis and Applications of Benzimidazole and Its Derivatives**" summarizes the general and special methods of synthesis of benzimidazole derivatives as well as a scheme of applications of these compounds in the areas of medicine, pharmacology, and chemistry, among

their use as catalysts or as ligands.

applications. It is organized as follows:

Section II: **Chemistry of Benzimidazoles**

and allergies, as well as for pain management.

Section III: **The Therapeutic Potential of Benzimidazoles**

tive of gliclazide. Preclinical and clinical studies are also discussed.

various catalytic systems.

others.
