Preface

This book consists of many chapters on different topics in the field of the latest research in quinazolinone and quinazoline derivatives.

The aim is to focus on all the methods for the synthesis and different interesting biological activities of quinazolinone and quinazoline derivatives.

The major objective of this book is to present the information in a lucid, condensed, and cohesive form, and to cater especially to the needs of readers in medicine and pharmacy.

The book has seven chapters from authors all over the world and covers the following topics:

• Introductory Chapter: The Newest Research in Quinazolinone and Quinazoline Derivatives

• Biological Activity of Quinazolinones

**II**

**Chapter 7 107**

Quinazoline Based Synthesis of some Heterocyclic Schiff Bases

*by Sainath Bhanudas Zangade*

• Synthesis of Quinazoline andQuinazolinone Derivatives

• 4(3H)-Quinazolinone Derivatives: Syntheses, Physical Properties, Chemical Reaction, and Biological Properties

• Quinazolinone and Quinazoline Derivatives: Synthesis and Biological Application

• Synthesis and Pharmacological Research Regarding New Compounds with Quinazolin-4-One Structure

• Quinazoline Based Synthesis of some Heterocyclic Schiff Bases

Many thanks go to all the authors for their valuable, interesting, and important research into quinazolinone and quinazoline derivatives.

The cooperation of the publisher IntechOpen is very much appreciated in publishing this book. The assistance received from Ms. Jasna Bozic, Author Service Manager, cannot be ignored. Any suggestions, comments, and criticisms on the subject matter will be gratefully acknowledged to improve future editions. My hope is that this work will prove to be a benefit to students and teachers of pharmacy and science, and to medical scientists.

**Dr. Ali Gamal Al-kaf** Professor, Medicinal Chemistry Department, Chief Council for Accreditation and Quality Assurance, Member of Higher Yemeni Medical Council, Previous Dean of Faculty of Pharmacy-Sana'a University, Yemen

**1**

Section 1

The Newest Research

in Quinazolinone and

Quinazoline Derivatives

Section 1

The Newest Research in Quinazolinone and Quinazoline Derivatives

**3**

**Figure 1.**

*The structure of the compound febrifugin (dichroin).*

**Chapter 1**

*Ali Gamal Al-kaf*

**1. Introduction**

Introductory Chapter: The Newest

Target searching for new high effective medicinal preparation is considered one of the actual problems of the modern public health. From medicinal preparations are the natural and synthetic origins of quinazolinone-4 derivatives. Quinazolinone derivatives are reported to be physiologically and pharmacologically active [1]. They also exhibit a wide range of activities such as anticonvulsant, antiinflammatory, antifungal, antimalarial, and sedative. Some of these compounds are identified as drugs used as diuretics, vasodilators, and antihypertensive agents. Moreover, sulfonamide derivatives have been widely used as bacteriostatic agents. Prompted by the abovementioned facts and in conjunction with our ongoing program on the utility of readily obtainable starting material for the synthesis of heterocyclic systems of biological interest, we have decided to synthesize a series of quinazolinone derivatives having sulfonamide moiety with potentially wide spectrum of biological responses [2, 3]. Information about the biological properties of derivatives of quinazolinone before the end of 60-years ago was more fragmentary. At the end of 40 years, an alkaloidal compound febrifugin (dichroin) 3-[β-keto-

γ(3-oxipiperidine-2) propyl] quinazolone-4 was isolated from Chinese plant Chang-Shan (Dichroa febrifuga Laur.) and has antimalarial activity, 100 times greater than quinine. This compound has not found clinical application, since it is

However, work with febrifugin encouraged further searching for new biologi-

Already, on early stages of the studies, chemotherapeutic, anti-inflammatory

Sixty to seventy years ago, more than 300 patents appeared in different countries, denoted synthesis and study of biological activity of this type of compounds. More than 20 medicinal preparations (analgesic, sedative, diuretic, hypotensive,

300 times toxic than quinine alkaloids [4, 9, 10, 21] (**Figure 1**).

activity, and hypnotic and hypotensive actions were revealed [5].

cally active compounds among the derivatives of quinazolinones-4 [4].

Research in Quinazolinone and

Quinazoline Derivatives

### **Chapter 1**
