I= SYNTHESIS OF 7-AZAINDOLE AND NICOTINAMIDE DERIVATIVES HAVING POTENTIAL THERAPEUTIC ACTIVITY
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Title of Thesis
SYNTHESIS OF 7-AZAINDOLE AND NICOTINAMIDE DERIVATIVES HAVING POTENTIAL THERAPEUTIC ACTIVITY

Author(s)
S. Moazzam Haider
Institute/University/Department Details
University of Karachi/Department of Pharmaceutical Chemicstry
Session
1995
Subject
Chemistry
Number of Pages
188
Keywords (Extracted from title, table of contents and abstract of thesis)
7-azaindole derivatives, nicotinamide derivatives, therapeutic activity, aromatic systems

Abstract
Pharmacology of heterocyclic compounds containing aromatic systems received great attention in the past decades for their physiological and therapeutic responses and their increasing use in the synthesis of specifically functionalized non-aromatic heterocyclic compounds.

In our present doctoral dissertation a study has been made on 7-azaindole and nicotinamide derivatives involved in the search for new pharmaceutical agents. To facilitate its readership we have designed this thesis into two parts, viz part A and part B. Part A constitutes the preparation and biological studies on thirteen derivatives of 7-azaindole (1-H-Pyrrolo (2.3-b) pyridine) while Part B, encompasses the synthesis of twelve derivatives of nicotinamide and ten derivatives of hexahydronicotinamide.

We have endeavoured our level best to approach biological activities in both parts. Biological activities are noted for each compound and are concisely discussed with respect to structure activity relationship. The introductory chapters provide a general over view of earlier contributions made in the field of chemistry and pharmacology of analogues of 7-azaindole and nicotinamide.

All the compounds were evaluated for their effects on mean arterial blood pressure on normotensive anaesthetized rats. Most of them showed hypotensive response at the dose of 10 mg/kg body weight.

Few derivatives which exhibited potent hypotensive activity in the respective series were selected for study of their effects on brain monoamines levels. These compounds showed significant change in catecholemines and indoleamines levels in whole brain of male albino mice and dose of 100 mg/kg.

The spectroscopic techniques such as 1H-NMR, EIMS, UV and IR were utilized for structure elucidation of the compounds.

Download Full Thesis
1072.23 KB
S. No. Chapter Title of the Chapters Page Size (KB)
1 0 Contents
54.69 KB
2 1 Part A - Introduction 5
81.76 KB
3 2 Experimental 18
164.42 KB
4 3 Discussion 46
229.62 KB
5 4 References 76
68.64 KB
6 5 Part B - Introduction 86
81.39 KB
7 6 Experimental 99
149.26 KB
8 7 Discussion 125
327.15 KB
9 8 References 168
76.36 KB
10 9 Appendix
74.45 KB
  9.1 List of Tables (Part A) 180
  9.2 List of Tables (Part B 181
  9.3 List of Substances (Part A) 183
  9.4 List of Substances (Part B) 184
  9.5 List of Figures (Part A) 186
  9.6 List of Figures (Part B) 187