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Title of article :
Synthesis and evaluation of uterine relaxant activity for a novel series of substituted p-hydroxyphenylethanolamines Original Research Article
Author/Authors :
C.L. Viswanathan، نويسنده , , A.S. Chaudhari، نويسنده ,
Issue Information :
روزنامه با شماره پیاپی سال 2006
Pages :
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Abstract :
Novel racemic 1-(4-hydroxyphenyl)-2-[3-(substituted phenoxy)-2-hydroxy-1-propyl]aminopropan-1-ol hydrochlorides (9a–h) were synthesized by condensing racemic 1-(p-hydroxyphenyl)-2-aminopropan-1-ol hydrochloride (6) with substituted aryloxymethyloxiranes (8a–h) in DMF in presence of anhydrous potassium carbonate and then reacting with dry hydrogen chloride gas. They were evaluated for uterine relaxant activity in vitro on isolated rat uterus and in vivo in pregnant rats. Their cAMP releasing potential was studied using rat uterus tissue homogenates by cAMP [3H] assay and cardiac stimulant potential was evaluated in dog. All compounds exhibited potent uterine relaxant activity in vitro and produced a significant delay in the onset of labour in pregnant rats; their cAMP releasing potential was higher than isoxsuprine hydrochloride except for 9b and 9c. Finally insignificant cardiac stimulant potential was noted for these compounds when compared to isoxsuprine hydrochloride.
Keywords :
Uterine relaxants , ?2-Adrenoceptor stimulants , Phenylethanolamines
Journal title :
Bioorganic and Medicinal Chemistry
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