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العنوان
Design and synthesis of some indole derivatives of expecting analgesic and anti-inflammatory activity /
المؤلف
Fouda, Mohamed Said Abdelhamid Said.
هيئة الاعداد
باحث / Mohamed Said Abdelhamid Said Fouda
مشرف / Mohamed El Husseiny El Sadek
مشرف / Samia Mahmoud Mostafa
مشرف / Ismail Awadalla Salama
الموضوع
Analgesics. Indole. .Medicinal chemistry
تاريخ النشر
2015.
عدد الصفحات
187 P. :
اللغة
الإنجليزية
الدرجة
ماجستير
التخصص
الصيدلة ، علم السموم والصيدلانيات
تاريخ الإجازة
1/1/2015
مكان الإجازة
جامعة قناة السويس - كلية الصيدلة - Medicinal Chemistry
الفهرس
Only 14 pages are availabe for public view

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from 187

Abstract

The present investigation comprises a survey covering the chemistry and the
biological activities of some compounds containing the indole ring system.
 In this work, diclofenac sodium was used as a precursor to obtain
compounds with higher activity and selectivity towards COX-2 enzyme.
Acid catalyzed cyclization for diclofenac sodium used to obtain the indole
ring.One known and five novel intermediate compounds were prepared, in
addition to twenty nine novel final compounds, a detailed discussion of the
experimental results attained is presented with an adequate interpretation.
 The new compounds were subjected to a molecular modeling simulation
study using Molegro Virtual Docking software (MVD), to predict their antiinflammatory
activity and selectivity towards COX-2 enzyme.
 Finally, all final compounds were subjected to in vivo evaluation of
analgesic activity using acetic acid induced writhing method, and antiinflammatory
activity using carrageenan induced paw edema, as well as
ulcerogenicity via oral administration of test compounds, the results revealed
that compounds V1, V5, V10, VI1, VI5, VI6, VI8, VI9, VI11, VIII2, IX2, and IX4
were the most active.