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SYNTHESIS OF 7-AZAINDOLE AND NICOTINAMIDE DERIVATIVES HAVING POTENTIAL THERAPEUTIC ACTIVITY

Haider, S. Moazzam (1995) SYNTHESIS OF 7-AZAINDOLE AND NICOTINAMIDE DERIVATIVES HAVING POTENTIAL THERAPEUTIC ACTIVITY. PhD thesis, University of Karachi, Karachi.

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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.

Item Type:Thesis (PhD)
Uncontrolled Keywords:7-azaindole derivatives, nicotinamide derivatives, therapeutic activity, aromatic systems
Subjects:Physical Sciences (f) > Chemistry(f2)
ID Code:616
Deposited By:Mr. Muhammad Asif
Deposited On:09 Sep 2006
Last Modified:04 Oct 2007 21:01

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