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العنوان
Novel Imidazole and Imidazolidinedione Derivatives :
المؤلف
Bass, Amr Kamal Abd El-Mageed.
هيئة الاعداد
باحث / عمرو كمال عبدالمجيد باص
مشرف / عمر محمد على
مشرف / منتصر شيخون أحمد
مشرف / عادل أحمد مرزوق
الموضوع
Pharmaceutical chemistry. Chemistry, Pharmaceutical.
تاريخ النشر
2016.
عدد الصفحات
141 p. :
اللغة
الإنجليزية
الدرجة
ماجستير
التخصص
العلوم الصيدلية
تاريخ الإجازة
19/9/2016
مكان الإجازة
جامعة المنيا - كلية الصيدلة - الكيمياء الطبية
الفهرس
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Abstract

The present study deals with the design and synthesis of novel imidazolidinedione derivatives and novel imidazole derivatives. It also includes evaluation of the anticonvulsant activity, neurotoxicity of all novel synthesized compounds and the anti-proliferative (cytotoxic inhibitory) activities of some selected compounds. The thesis includes four main sections; introduction, scope of investigation, results & discussion and the experimental sections in addition to references and abstract.
The first section “Introduction” includes an overview about the synthetic procedures of imidazoles and imidazolidinediones and their biological activities.
As a result of these aspects, the second part “Scope of investigation” outlines the main goals and the rationale of this work. The ideas employed in designing novel and potent anticonvulsant compounds with the lowest neurotoxicity. The aim of this work is achieved via the synthesis of series of novel imidazolidinedione derivatives and novel 1,2,4,5-tetra substituted imidazole derivatives with the objective of discovering their anticonvulsant activity.
Also, in this work, the cytotoxic inhibitory activity of some selected target compounds from all series was evaluated.
For the purpose of achieving these goals, the third section entitled “Results and discussion” discusses and describes the data obtained from the various steps of synthesis of imidazolidinediones series I (3a-e) and series II (4a-e) as well as synthesis of imidazoles series III (9a-e), series IV (10a-e) and series V (11a-e), structural elucidation of newly synthesized compounds is based on different spectral methods and elemental analysis
Also in this section, another part discusses and describes the data obtained from biological evaluation; the anticonvulsant evaluation indicated that the activity of the target compounds against MES induced seizures were less than that of phenytoin and all the compounds were effective in s.c. PTZ screen. The results of neurotoxicity screening indicated that most of compounds under investigation were devoid of toxic effect.
Evaluation of the anti-proliferative (cytotoxic inhibitory) activities results revealed that the majority of the selected compounds have from moderate to weak activity against the most of cell lines tested.
The fourth section, “Experimental”, is divided into two parts;
A) The different procedures employed in synthesis of the targeted compounds and presented all detailed spectroscopic and analytical data of the novel compounds that are 25 new compounds.
B) The biological evaluation part which is subdivided into:
i) Evaluation of the anticonvulsant activity and neurotoxicity of all newly synthesized compounds (series I, series II, series III, series IV and series V) with respect to that of valproate sodium and phenytoin sodium as reference drugs according to the protocol given by the epilepsy section of National Institute of Neurological Disorders and Stroke (NINDS) using the standard protocol adopted by the Antiepileptic Drug Development (ADD) program which includes the maximal electroshock seizure (MES) screen, the subcutaneous pentylenetetrazole (s.c.PTZ) screen and the rotarod (neurotoxicity) test.
ii) Evaluation of the in vitro anti-proliferative activity; this part described the process and methodology followed by the National Cancer Institute for evaluation of the anticancer activity of the selected compounds 3e, 4c-e, 9a, 9d, 10a-e and 11e.