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العنوان
Synthesis of some thiophene derivatives of expected anti-inflammatory activity /
الناشر
Ahmed Abdelmohsen Abdellatif Ibraheem ,
المؤلف
Ahmed Abdelmohsen Abdellatif Ibraheem
هيئة الاعداد
باحث / Ahmed Abdel Mohsen Abdel Latif Ibraheem
مشرف / Salwa Elsayed Mohamed Elmeligie
مشرف / Nadia Abdalla Khalil
مشرف / Hala Bakr Elnassan
تاريخ النشر
2020
عدد الصفحات
158 P . :
اللغة
الإنجليزية
الدرجة
الدكتوراه
التخصص
الصيدلة ، علم السموم والصيدلانيات (المتنوعة)
تاريخ الإجازة
25/1/2020
مكان الإجازة
جامعة القاهرة - كلية الصيدلة - Pharmaceutical Organic Chemistry
الفهرس
Only 14 pages are availabe for public view

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from 188

Abstract

This thesis comprises five chapters. The first chapter is an introduction, which highlights the pharmacological importance of some thieno[3,2-d]pyrimidine derivatives, and briefly reviews the different synthetic strategies used for their synthesis. Further, it touches on the role of p38Ü mitogen activated protein kinase (MAPK) in inflammation, its tertiary structure, and its inhibition using small molecule inhibitors. The second chapter demonstrates the aim of this work along with proposed Schemes detailing the pathways used for the synthesis of the starting materials, intermediates, and the new target compounds. Scheme 1 illustrates the synthesis of the intermediate compounds IIIa-c and IVa-k. Nitration of p-toluidine and p-anisidine using urea nitrate afforded the corresponding 3-nitro derivatives Ib, c. The latter compounds, along with the commercially available 3-nitroaniline (Ia), were reacted with benzoyl chloride to afford the corresponding benzamides IIa-c, which were subsequently subjected to iron-catalyzed reduction reaction to give the benzamides IIIa-c. Reaction of the latter as well as some commercially available substituted anilines, with chloroacetyl chloride afforded 2-chloro-N-(substituted phenyl)acetamides IVa-k.Scheme 2 describes the synthesis of the tetrasubstituted thiophenes VIIa-g, VIII and IXa-k starting with bis(methylsulphanyl)methylenemalononitrile (V), which was reacted with phenylpiperazine and Na2S·9H2O to give the thioamide derivative VI. The latter was subjected to S-alkylation followed by Thorpe-Ziegler cyclization using commercially available phenacyl bromides, ethyl chloroacetate, and 2-chloroacetamides IVa-k to afford VIIa-g, VIII, and IXa-k, respectively