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العنوان
Synthesis and Biological Evaluation of Some Novel Substituted Quinazoline Derivatives /
المؤلف
Ahmed, Eman Gaber Sayed.
هيئة الاعداد
باحث / إيمان جابرسيد أحمد
مشرف / صافيناز السيد عباس
الموضوع
Pharmaceutical Chemistry.
تاريخ النشر
2012.
عدد الصفحات
p 150. :
اللغة
الإنجليزية
الدرجة
ماجستير
التخصص
العلوم الصيدلية
تاريخ الإجازة
20/5/2012
مكان الإجازة
جامعة بني سويف - كلية الصيدلة - اكيمياء الصيدلية
الفهرس
Only 14 pages are availabe for public view

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Abstract

Quinazoline derivatives received considerable interest as they are associated with a wide range of biological activities.
This thesis pointed towards the anticonvulsant and antiinflammatory activities of 2-(2,4-dichlorophenoxymethyl) 3-substituted quinazolin-4(3H)one derivatives. In the present work, the new compounds were designed and synthesized depending on the incorporation of several structural features and functional groups that are believed to positively contribute to the anticonvulsant or antiinflammatory properties hoping to reach derivatives of high potency and low side effects.
This thesis consists of the following parts:
1. Introduction:
In this section, a literature review about the various biological and pharmacological activities of quinazolines is presented.
2. Aim of the work:
It includes the research objectives and the major aims that direct the theoretical and practical work.
3. Discussion:
It deals with the discussion of the experimental methods adopted for the synthesis of the designed compounds with a summarized data about the characterization of these new compounds.
4. Experimental:
In this part, the practical procedures adopted for the synthesis of the reported and new intermediates as well as the new final compounds are presented. In addition, their spectral and elemental microanalytical data are cited.
5. Pharmacological Screening:
a. Anticonvulsant Screening:
All new compounds and intermediates designed and prepared in schemes 1 and 2 (20 compounds) were evaluated for their anticonvulsant activity using two methods:
i. Strychnine-induced seizures where 8 compounds (IVe, Vc, Vd, VI, VII, VIII, IXc and Xb) exhibited anticonvulsant activity but less than that of the reference drug phenobarbitone sodium. Toxicity study was performed on the most active compounds.
ii. Maximal electroschock-induced seizures (MES) where 4 compounds (IVd, Ve, VIII and Xa) showed a nearly equipotent anticonvulsant activity compared to the reference drug phenytoin. Also, 4 compounds (Vb, Vd, IXb and Xc) were more active than phenytoin.
b. Antiinflammatory Screening:
All new compounds and intermediates designed and prepared in scheme 4 (24 compounds) were evaluated for their antiinflammatory activity using ”rat paw carrageenan oedema” method. Two compounds XIVf and XIVg were equipotent to the reference drug diclofenac-sodium. Also, 9 compounds (XIa, XIIIc, XIVa, XIVh, XIVi, XVb, XVc, XVd and XVe) showed significant activity (80%-94%).
The ulcerogenic potential was determined for the most active compounds (XIa, XIVa, XIVf, XIVg, XIVh, XIVi, XVb, XVd and XVe) and they were found to be safer than diclofenac-sodium.
6. References:
This part includes 135 references covering the period 1962-2011.