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SYNTHESIS OF SOME PIPERIDINE DERIVATIONS OF POTENTIAL BIOLOGICAL INTEREST

Siddiqui, Hanifa Shahnaz (1997) SYNTHESIS OF SOME PIPERIDINE DERIVATIONS OF POTENTIAL BIOLOGICAL INTEREST. PhD thesis, University of Karachi, Karachi.

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Abstract

Present work includes the synthesis of piperidine derivatives having potential therapeutic activities. Pethidine and morphine like compounds are well known for exhibiting agonistic as well as antagonistic activities. Molecular modifications of these compounds led to new opiates or narcotics analgesic. Piperidine is one of the most important heterocycles which exhibits many therapeutic activities due to its conformational flexibility. Minor alterations in the chemical structure have shown considerable change in the activities. During the course of present work substituted phenacyl derivatives of methyl 4hydroxy piperidine were synthesized. The analgesic and neurochemical activities were studied. The analgesic activities were determined by thermal method. Most of the compounds exhibited analgesic activity when evaluated by thermal method. The effects of these newly synthesized derivatives are studied on brain mono amines levels. These compounds showed significant change in catecholamines and indolemines level in whole brain male albino mice at doses of 100 mg/kg body weight. The cytotxicity of these compounds was determined against Artimia salina by brine shrimp bioassay. Few derivatives exhibited promising cytotoxicity. The effects of these derivatives on smooth muscles (vivo and vitro) were also studied in Guinea pigileum and Rabbit Jejunum. Non of the compound showed activity upto a very high range 3mM. Spectroscopic techniques such as 1H-NMR,EIMS, UV and IR were utilized for characterization and structure confirmation of the compounds.

Item Type:Thesis (PhD)
Uncontrolled Keywords:piperidine derivations, piperidine, therapeutic activities, pethidine, morphine, analgesic activities, neurochemical activities
Subjects:Biological & Medical Sciences (c) > Biological Sciences(c1) > Biology (c13)
ID Code:1252
Deposited By:Mr. Muhammad Asif
Deposited On:02 Feb 2007
Last Modified:04 Oct 2007 21:05

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