Document Details

Document Type : Project 
Document Title :
: Design and synthesis of aryloxyalkylamines as h5-HT1B agonist to be tested as analgetics with possible anti-migraine activity
تصميم و تحضير مشتقات الاريلوكسىالكيل امين كمماثلات للسيراتونين لاختبار تأثيرها كمسكنات مع احتمال استخدامها كمضادات للصداع النصفي
 
Subject : Pharmaceutical Chemistry 
Document Language : Arabic 
Abstract : Development of drugs acting on h5-HT1b serotonin subreceptors represents an exciting new area of research as a result of the increasing attention of the involvement of these receptors in psychiatric disorders. Most of h5-HT1b serotonin subreceptors agonists bind with high affinity but with low selectivity. Aryloxyalkylamines are curious exception. For example propranolol (I) binds with high affinity at r5-HT1B receptors but displays low affinity at h5-HT1b receptors. Structure modifications of (I) resulted in (II) that binds with high affinity at h5-HT1b. These findings encourage us to undertake further study, in which, we design and synthesize a new series of aryloxyalkylamines (4, 5, 8-13 and 16-17), in which, a- the alkyl side chain is ethyl or substituted ethyl at α- or β-carbon by methyl or phenyl keeping the distance between O and N atoms as in (II), b- the naphthyl moiety is replaced by phenyl group substituted at 2,3-, 2,4-, 2,5-, or 2,6- positions by halogens. The structures of the new compounds are confirmed by microanalyses and 1H-NMR spectroscopy. The lipophilic characters of the prepared compounds are calculated. Some of them are subjected to 3D studies and were found to be superimposed on compound (II). The binding affinity, for most of the compounds, at 5-HT1b and 5-HT1d were determined and some were found to bind with high affinity and selectivity compared to (I) and with comparable affinity and selectivity to (II). The analgetic activity of selected compounds were determined on experimental animals and proved to have 66-100% analgetic activity compared to aspirin 
Publishing Year : 1425 AH
2005 AD 
Sponsor Name : kau 
Sponsorship Year : 1425 AH
2005 AD 
Added Date : Saturday, November 7, 2009 

Researchers

Researcher Name (Arabic)Researcher Name (English)Researcher TypeDr GradeEmail
عبد القادر مختار إسماعيلIsmaie, Abdelkader MokhtarInvestigatorDoctorate 

Files

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 24394.doc doc 

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