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العنوان
Synthesis of some new pyrazole derivatives of pharmaceutical interest /
المؤلف
Harmal, Ammar Nasser Omi Saleh.
هيئة الاعداد
باحث / Ammar Nasser Omi Saleh Harmal
مشرف / Abd-El-Galil Mohamed Khalil
مشرف / Mohamed Abbas El-Metwally
مشرف / Moustafa Ahmed Gouda
الموضوع
pyrazole derivatives.
تاريخ النشر
2012.
عدد الصفحات
247 p. :
اللغة
الإنجليزية
الدرجة
ماجستير
التخصص
الكيمياء
تاريخ الإجازة
1/1/2012
مكان الإجازة
جامعة المنصورة - كلية العلوم - Department of Chemistry.
الفهرس
Only 14 pages are availabe for public view

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from 247

Abstract

.1Introduction to the chemistry of aminopyrazolesThe chemistry of aminopyrazoles has been extensively investigated in the past.The considerable biological and medicinal activities of pyrazoles, andazolopyrazoles, for which aminopyrazoles are preferred precursors, havestimulated these investigations. Interest in aminopyrazole synthesis and
chemistry has recently been reviewed.
2- Original article
Synthesis, antitumor, cytotoxic and antioxidant evaluation of some new
pyrazolotriazines attached to antipyrine moiety
a b s t r a c t
Iminopropanehydrazonoyl cyanide 4 was achieved upon reaction of antipyrinediazonium salt 2 with 3-iminobutanenitrile (3) in EtOH/AcONa. 3-Aminopyrazole derivative 5 was obtained upon reaction of 4 with hydrazine hydrate. Diazodization of 5 afforded the diazonium salt 6 which coupled with active methylene compounds 7e10, 19, 20, 25, 29 and 32 in pyridine to give aryl hydrazone derivatives 11e14, 21, 22, 26, 30 and 33, respectively. Refluxing of compounds 11-14, 21, 22, 26 and 33 in acetic acid afforded the pyrazolotriazines 15e18, 23, 24, 28 and 35, respectively. The newly synthesized compounds
were screened for their cytotoxic and antioxidant activities. The results showed clearly that compounds 4, 5, 13, 22, and 24 displayed promising in vitro anticancer activity against four different cell lines (HepG2, WI 38, VERO and MCF-7). Compounds 4 and 22 are the more potent antioxidant and anticancer agents. On the other hand, most of the compounds exhibited good cytotoxic activity toward (EAC.
Article-3
3-Iminobutanenitrile as Building Block for the Synthesis ofSubstituted Pyrazolo[1,5-a]pyrimidines with Antitumor andAntioxidant Activities.
Abstract: Iminopropanehydrazonoyl cyanide 4 was obtained by diazotization of
antipyrinyldiazonium salt 2 and 3-iminobutanenitrile (3) in EtOH/AcONa. 3-
Aminopyrazole 5 was obtained by reaction of 4 with hydrazine hydrate in 1,4-dioxane.
Diazodization of 5 afforded the diazonium salt 6 which coupled with pyrazole 7 to give
pyrazolo-pyrimidine 15. Furthermore, compound 5 was used as a key intermediate for the
synthesis of pyrazolopymidines37-39, 41, 42,48a, b, 52, 53 and 55-59 via its reaction with
1,3-diketone, halocarbonyl, aryledines and DMF-DMA followed by reaction with active
methylene components. Newly synthesized compounds were screened for their antitumor
and antioxidant activities. The obtained results showed clearly that most of compounds
exhibited good antitumor activities and weak antioxidant activities, while compounds 4 and
exhibited broad spectrum of antitumor and antioxidant activities.