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العنوان
Synthesis and Biological Screening Of Some Heterocyclic Derivatives as Antiprozoal Agents /
المؤلف
ElSeidy, Aya Mohamed Mosatafa.
هيئة الاعداد
باحث / اية محمد مصطفى الصعيدى
مشرف / عدنان احمد بخيت
مشرف / منال نبيل سعيد سعودى
مشرف / احمد مصطفى محمد حسن
مشرف / سلوى محمد حسن فهمى
الموضوع
Pharmaceutical Chemistry. Heterocyclic - Derivatives. Antiprozoal Agents.
تاريخ النشر
2017.
عدد الصفحات
195 p. :
اللغة
الإنجليزية
الدرجة
ماجستير
التخصص
الصيدلة
تاريخ الإجازة
11/4/2017
مكان الإجازة
جامعة الاسكندريه - كلية الصيدلة - الكيمياء الصيدلية
الفهرس
Only 14 pages are availabe for public view

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Abstract

It is well known that pyrazole ring whether free or hybridized with other heterocyclic rings displayed a wide array of biological activities, such as antibacterial, antiviral, antitubercular, anti-inflammatory, antioxidant, anticancer, antimalarial and antileishmanial. It was found that currently used antimalarial and antileishmanial drugs are suffering from several drawbacks such as, rapidly developed resistance and severe adverse effects. Therefore, there is a crucial need to synthesize new derivatives which target novel pathways and enzyme inside protozoa with large margin of safety.
<In the present study, we shed some light on the antimalarial and antileishmanial activity of pyrazole ring so we selected 1,3-diaryl pyrazole derivatives with known antiprotozoal activity.
After that, some modifications on the parent nucleus were performed to form open chain and hybridized derivatives. Then, only molecules with high binding affinities and docking score in the computational docking studies were synthesized and further investigated for the effect of such molecular variations on their biological activities.
<This thesis consists of the following:
1. Introduction It represented a brief overview on some protozoal diseases such as, malaria and leishmania giving some details about their global distributions, life cycles of associated protozoa, currently used drugs and development of resistance. There was also a literature survey on biologically active pyrazole derivatives which exhibited antimalarial and antileishmanial activities focusing on only recent researches.
2. Research Objectives It clarified the aim of the present work and rational upon which the target compounds were designed, synthesized and biologically screened for their antimalarial and antileishmanial activities.
<3. Results & Discussion It included three parts; chemistry, biological screening and molecular modeling 3.1. Chemistry It described the different practical methods adopted for synthesis of starting, intermediate and final designed compounds with referenc to the available literature, as well as elucidation of their structures using elemental microanalyses and various spectroscopic techniques such as, IR, 1H-NMR, 13C-NMR and mass spectra.