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العنوان
Synthesis of Some New Organo-Complexes Containing New Pyrazolopyridine Derivatives with Expected Biological Activity /
المؤلف
.Amer, Mona Mohamed Mohamed El-Shikh
هيئة الاعداد
باحث / مني محمد الشيخ عامر
مشرف / فرج عبد الله العيسوي
مشرف / سعيدة ابو الثثنا ابو العنين
مناقش / ممدوح سعد مسعود
الموضوع
Pesticides. Agricultural chemicals. Pests- Biological control.
تاريخ النشر
2014.
عدد الصفحات
139 p.
اللغة
الإنجليزية
الدرجة
ماجستير
التخصص
Biochemistry
تاريخ الإجازة
1/2/2014
مكان الإجازة
جامعة المنوفية - كلية العلوم - قسم الكيمياء
الفهرس
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Abstract

The entitled thesis ”synthesis of some new organo-complexes
containing new pyrazolopyridine derivatives with expected biological
activity” comprises three chapters:
Chapter I includes the literature review about synthesized and biological
activity of 1H-pyrazolo[3,4-b]pyridine compounds and complex
formation studies of some pyrazolo-pyridine derivatives.
Chapter II is concerned with the experimental part ten derivatives were
prepared and characterized six metal complexes derived from 2-(3-
amino-4,6-dimethyl-1H-pyrazolo[3,4-b]pyridin-1-yl)aceto-hydrazide
were prepared and analyzed. Different standardized instruments were
used for obtaining the required data (spectral method UV-vis., IR, HNMR,
C13-NMR, mass spectra) magnetic susceptibility, molar
conductivity and thermogravimetric analysis TGA and also molecular
modeling and docking studies were performed for some of the
synthesized compounds in order to predict there biological activities
toward AKR1C3 complexed with its bound inhibitor Indomethacin using
Molsoft ICM 3.4-8C program. The ICM scores are good enough to
design future anticancer agents with therapeutic potentials.
Chapter III collects the results and discussions and divided into two
subdivisions:
III.1. The first subdivision involves the synthesis and characterization of
number of new N-alkylated and 1,2,4-triazole, 1,3,4-oxa-, thiadiazoles
including 4,6-dimethyl-1H-pyrazolo[3,4-b]pyridin-3-amine were
synthesized. The starting material 4,6-dimethyl-1H-pyrazolo[3,4-
b]pyridin-3-amine (1) was alkylated, after its treatment with anhydrous
potassium carbonate in dry N,N-dimethylformamide, with ethyl-2-
bromoacetate to give ethyl 2-(3-amino-4,6-dimethyl-1H-pyrazolo[3,4-b]pyridin-1-yl)acetate (2) in good yield. The latter derivative 2 was
treated with hydrazine hydrate, in ethanol on boiling, to afford the
corresponding acid hydrazid. 2-(3-Amino-4,6-dimethyl-1H-pyrazolo[3,4-
b]pyridin-1-yl)acetohydrazide (3) was cyclized on treating with carbon
disulfide, in basic medium, to give the 5-((3-amino-4,6-dimethyl-1Hpyrazolo[
3,4-b]pyridin-1-yl)methyl)-1,3,4-oxadiazole-2-thiol (4). the
latter oxadiazole 4 was also elucidated via its alkylation reactions with
some alkylation agents such as methyl, ethyl iodide and benzyl chloride
to afford the S-alkyl derivatives 5a-c. These alkylated derivatives were
elucidated by the MS spectra which showed the molecular ion peaks
corresponding to its molecular weights (Scheme 1).