Sunday , 17 January 2021

A COMPREHENSIVE REVIEW ON SUBSTITUTED QUINAZOLINONES AND ITS DERIVATIVES

About author :
Ramesh Dhani
Department of Pharmaceutical Chemistry
JNTUA-OTRI, Anantapur, India
E-mail: dhanipharmachem@gmail.com
ABSTRACT:
Quinazolinone is a heterocyclic chemical compound. There are two structural isomers, 2-quinazolinone and 4-quinazolinone, with the 4-isomer being the more common. Quinazolinones and several of their derivatives have been found to be of greater interest in view of their varied biological and pharmacological properties. The present survey aims to achieve the synthesis of quinazolinones and their derivatives of specific pharmacological properties: sedative hypnotics and anti-Convulsants, anti-Parkinsonial agents, Diuretics, and Chemotherapeutic agents like anti-Viral, anti-Bacterial, anti-Helintics, anti-Malarial, anti-Cancer, Smooth Muscle Relaxants, anti-Hypertensive agents, Analgesics and anti-Inflammatory agents, hypoglycemic agents, anti-Histaminics. This paper proves to be significant for further research work on the bioactive quinazolinone ring.
Key words: Quinazolinone, Anthranilic acid, Acetyl chloride, Ethanol, Anti-Helintics, Anti-Malarial, Anti-Cancer.
Introduction:
The practice of medicinal chemistry is devoted to the discovery and development of new agents for treating diseases most of the activity in this discipline is direct to new synthetic or natural organic compounds, but organic compounds with increasingly specific pharmacological activities are clearly the dominant force
Quinazoline  is a bicyclic compound earlier known as benzo-1,3-diazine was prepared in the laboratory by Gabriel in 1903 although one of its derivative was known much earlier The name quinazolinone was proposed for its compound by Weddige, on observing that this was isomeric with the then compound cinnolineand quinaoxaline. The numbering of the quinazoline ring system which is currently used was suggested by Paal and Busch.
Synthesis :
Quinazoline in 1905 Riedel obtained a patent describing a synthesis of quinazoline from o-nitrobenzaldehyde through reaction with formamide to the o-nitrobenzylidene  diformamide. Reduction of this with zinc and dilute acetic acid gave quinozoline in good yield. Later improvements in Riedel’s original procedure to obtain up to 65% overall yield have been reported. This is the best method of obtaining quinazoline. It suffers only from the difficulty of obtaining o-nitrobenzaldehyde and especially substituted o-nitrobenzaldehydes. It has been applied to substitute quinozolines, for the preparation of 6,7-dimethoxy quinazoline through the intermediate 6-nitroveratradehyde
Pharmacological Activity:
Quinazolinones and several of their derivatives have been found to be of greater interest in view of their varied biological and pharmacological properties. The present survey aims to achieve the synthesis of quinazolinones and their derivatives of specific pharmacological properties: sedative hypnotics and anti-Convulsants, anti-Parkinsonial agents, Diuretics, and Chemotherapeutic agents like anti-Viral, anti-Bacterial, anti-Helintics, anti-Malarial, anti-Cancer, Smooth Muscle Relaxants, anti-Hypertensive agents, Analgesics and anti-Inflammatory agents, hypoglycemic agents, anti-Histaminics.etc
Ahmad R.Khosropour & Co-Workers(2006), Synthesized a new, efficient and reusable promoter system for the 4(3H)-Quinazolinones in high to excellent yields through the one-pot condensation of anthranilic acid, trimethyl orthoformate and primary amines in the presence of 5 mol % of Bi(TFA)3 immobilized on [nbp]FeCl4 as a room temperature ionic liquid.
Usha Ameta, & Co-workers(2006) reported A simple method for the syn- thesis of compounds and Synthetic studies on some 3-[(5-arylidene-4-oxo-1,3-thiazo-lidin-2-yliden)amino]-2-phenylquinazolin-4(3H)-ones & their ethoxy phthalimide derivatives
which were isolated from aseries of reactions. And the structure of isol -ated compounds has been determined by means of IR, 1H NMR and mass spectroscopy .

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