Synthesis and Biological Activity

*Quinazolinone and Quinazoline Derivatives*

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**Chapter 3**

**Abstract**

biological activity

**1. Introduction**

**2. Chemistry of quinazoline**

[8–10].

**41**

*Heba E. Hashem*

Synthesis of Quinazoline and

Active heterocyclic compounds are one of the main topics of interest for the medicinal chemists as they display a number of pharmacological activities. Nitrogen, sulfur, and oxygen containing five- and six-membered heterocyclic compounds have occupied enormous significance in the field of medicinal chemistry. The most important six-membered heterocyclic compounds are quinazoline and quinazolinone derivatives for their biological activities. The current chapter outlined the different methods for synthesis of quinazoline and quinazolinone

**Keywords:** quinazoline, quinazolinone synthesis, six-membered heterocycles,

Quinazoline (1,3-diazanaphthalene or 5,6-benzopyrimidine) and 4(3H) quinazolinone derivatives have a great interest in organic synthesis and medicinal chemistry fields as they possess a broad range of pharmacological activities. They exhibit antimicrobial [1], antimalarial [2], antioxidant [3], anti-inflammatory [4], anticonvulsant [5], antihypertensive [6], antidiabetic [7], and antitumor activities

Many quinazolinone derivatives occurred naturally in various classes of the plant kingdom, microorganisms, and different animals (**Figure 1**). The first discovery of quinazolinone alkaloid is *febrifugine* which possesses antimalarial potential,

Quinazoline is a heterocyclic compound of two fused six-membered simple aromatic rings—benzene and pyrimidine ring. It is a yellow-colored compound, found usually in crystalline form. Its oxo-derivative (quinazolinone) is classified into three types according to the position and number of carbonyl group: 2(1H) quinazolinones, 4(3H)quinazolinones, and 2,4(1H,3H)quinazolinedione (**Figure 2**).

Quinazoline is a compound made up of two fused six-membered simple aromatic rings—benzene and pyrimidine ring. The properties of the pyrimidine ring were affected by the presence of fused benzene ring. The two nitrogen atoms are not equivalent, and the marked polarization of the 3,4-double bond is reflected

extracted from the Chinese plant *aseru* (*Dichroa febrifuga* Lour) [11].

Quinazolinone Derivatives

derivatives that possess broad spectrum of biological activities.

### **Chapter 3**
