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العنوان
Synthwsis Of Some Quinazolinone Derivatives Fused Or Non-Fused To Heterocyclic Rings Of Potential Biological Activity /
المؤلف
El-sayed, Azza El-Sayed Ismail Ismail.
هيئة الاعداد
باحث / Azza El-sayed Ismail Ismail El-sayed
مشرف / Farid Soliman Gabra Soliman
مشرف / Aly Abou-Elfadl Hazzaa
مشرف / Ahmed Mostafa Mohamed Hassan
مشرف / Hayam Mohamed Abd-Elhady Ashour.
الموضوع
Pharmaceutical Chemistry.
تاريخ النشر
2013.
عدد الصفحات
119 p. :
اللغة
الإنجليزية
الدرجة
الدكتوراه
التخصص
العلوم الصيدلية
تاريخ الإجازة
4/8/2013
مكان الإجازة
جامعة الاسكندريه - كلية الصيدلة - Pharmaceutical Chemistry
الفهرس
Only 14 pages are availabe for public view

from 134

from 134

Abstract

It is well documented that the quinazolinone ring has a wide variety of activities, especially anti-inflammatory, antimicrobial, anticancer, anticonvulsant, and other miscellaneous activities.
Also, it has been reported that the substitution pattern by different aryl or heteroaryl moieties at positions 2 and 3 of the quinazoline nucleus markedly influences the anti- inflammatory activity. Moreover, a literature survey revealed that a dithiocarbamate moiety, a triazinan ring, and some azoles when incorporated into heterocyclic templates induce diverse biological activities.
The present thesis aimed at the synthesis and biological evaluation of new quinazolinone derivatives substituted at position 3 with the above-mentioned pharmacophoric moieties. In addition, novel pyrazolo[5,l-bjquinazolin-9(4R)-one derivatives -comprising the pyrazoloquinazoline scaffold either directly attached or linked through a small spacer to some heterocyclic moities- were synthesized to explore their anti-inflammatory and antimicrobial activities.
The present thesis comprises the following chapters;
Chapter 1: Introduction
This chapter includes a concise survey on the recent literature citing the activity of the quinazolinone ring as anti-inflammatory, antimicrobial, anticancer, and anticonvulsant agent. In addition, a number of miscellaneous activities are discussed.
Chapter 2: Research Objectives
Deals with the aim of the work, and the rationale upon which the new compounds have been synthesized.
Chapter 3: Discussion
This chapter deals with the discussion of the adopted synthetic routes to synthesize the target compounds.
The thesis comprises four synthetic schemes:
Scheme 1
Describes the preparation of 2-methylbenzo{dJ[l,3joxazin-4-one (Acetanthranil); 2, and its conversion to the key intermediate: 3-amino-2-methylquinazolin-4(3fl)-one; 3. This intermediate was converted to I -(2-methyl-4-oxoquinazolin-3 (41])-yl)-3- (substituted) phenyl thioureas; 4-6 using the appropriate isothiocyanate. The latter were cyclized using formalin! aminoacids to 2-methyl-3-[3-(phenyl; or 4-substituted phenyl) - 5-substituted-2-thioxo- 1,3 ,5-triazinan- 1 -yl) quinazolin-4(3R)-ones; 7-12.
The key intermediate 3-amino-2-methylquinazolin-4(3R)-one; 3 was then converted to its dithiocarbamate salt Potassium 2-methyl-4-oxoquinazolin-3(4F1)-ylcarbamodithioate; 13 using CS2/KOH.