SYNTHESIS AND AChE INHIBITING ACTIVITY OF 2, 4 SUBSTITUTED 6-PHENYL PYRIMIDINES

Novel substituted pyrimidines were synthesized from methyl 2,4-dioxo-4-phenyl-butanoate (I-A) and urea, followed by Mitsunobu coupling of I-A with benzyl or allyl alcohol to give the corresponding 2-hydroxypyrimidine ethers in good yields. Saponification of I-A, followed by reaction with benzyl or a...

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Autores principales:	PAZ,CRISTIAN, PETER,MARTIN G, SCHMIDT,BERND, BECERRA,JOSE, GUTIÉRREZ,MARGARITA, ASTUDILLO,LUIS, SILVA,MARIO
Lenguaje:	English
Publicado:	Sociedad Chilena de Química 2012
Materias:	Pyrimidines inhibition AChE mitsunobu TBTU
Acceso en línea:	http://www.scielo.cl/scielo.php?script=sci_arttext&pid=S0717-97072012000300020
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spelling	oai:scielo:S0717-970720120003000202019-02-19SYNTHESIS AND AChE INHIBITING ACTIVITY OF 2, 4 SUBSTITUTED 6-PHENYL PYRIMIDINESPAZ,CRISTIANPETER,MARTIN GSCHMIDT,BERNDBECERRA,JOSEGUTIÉRREZ,MARGARITAASTUDILLO,LUISSILVA,MARIO Pyrimidines inhibition AChE mitsunobu TBTU Novel substituted pyrimidines were synthesized from methyl 2,4-dioxo-4-phenyl-butanoate (I-A) and urea, followed by Mitsunobu coupling of I-A with benzyl or allyl alcohol to give the corresponding 2-hydroxypyrimidine ethers in good yields. Saponification of I-A, followed by reaction with benzyl or allyl amines in the presence of TBTU yielded 2-hydroxy-6-phenyl-pyrimidine 4-carboxamides. AChE and BuChE assays revealed 2-hydroxy-6-phenyl-pyrimidine-4-carboxyallyamide as the most active compound, IC50= 90 µM, with no inhibition of BuChE.info:eu-repo/semantics/openAccessSociedad Chilena de QuímicaJournal of the Chilean Chemical Society v.57 n.3 20122012-01-01text/htmlhttp://www.scielo.cl/scielo.php?script=sci_arttext&pid=S0717-97072012000300020en10.4067/S0717-97072012000300020
institution	Scielo Chile
collection	Scielo Chile
language	English
topic	Pyrimidines inhibition AChE mitsunobu TBTU
spellingShingle	Pyrimidines inhibition AChE mitsunobu TBTU PAZ,CRISTIAN PETER,MARTIN G SCHMIDT,BERND BECERRA,JOSE GUTIÉRREZ,MARGARITA ASTUDILLO,LUIS SILVA,MARIO SYNTHESIS AND AChE INHIBITING ACTIVITY OF 2, 4 SUBSTITUTED 6-PHENYL PYRIMIDINES
description	Novel substituted pyrimidines were synthesized from methyl 2,4-dioxo-4-phenyl-butanoate (I-A) and urea, followed by Mitsunobu coupling of I-A with benzyl or allyl alcohol to give the corresponding 2-hydroxypyrimidine ethers in good yields. Saponification of I-A, followed by reaction with benzyl or allyl amines in the presence of TBTU yielded 2-hydroxy-6-phenyl-pyrimidine 4-carboxamides. AChE and BuChE assays revealed 2-hydroxy-6-phenyl-pyrimidine-4-carboxyallyamide as the most active compound, IC50= 90 µM, with no inhibition of BuChE.
author	PAZ,CRISTIAN PETER,MARTIN G SCHMIDT,BERND BECERRA,JOSE GUTIÉRREZ,MARGARITA ASTUDILLO,LUIS SILVA,MARIO
author_facet	PAZ,CRISTIAN PETER,MARTIN G SCHMIDT,BERND BECERRA,JOSE GUTIÉRREZ,MARGARITA ASTUDILLO,LUIS SILVA,MARIO
author_sort	PAZ,CRISTIAN
title	SYNTHESIS AND AChE INHIBITING ACTIVITY OF 2, 4 SUBSTITUTED 6-PHENYL PYRIMIDINES
title_short	SYNTHESIS AND AChE INHIBITING ACTIVITY OF 2, 4 SUBSTITUTED 6-PHENYL PYRIMIDINES
title_full	SYNTHESIS AND AChE INHIBITING ACTIVITY OF 2, 4 SUBSTITUTED 6-PHENYL PYRIMIDINES
title_fullStr	SYNTHESIS AND AChE INHIBITING ACTIVITY OF 2, 4 SUBSTITUTED 6-PHENYL PYRIMIDINES
title_full_unstemmed	SYNTHESIS AND AChE INHIBITING ACTIVITY OF 2, 4 SUBSTITUTED 6-PHENYL PYRIMIDINES
title_sort	synthesis and ache inhibiting activity of 2, 4 substituted 6-phenyl pyrimidines
publisher	Sociedad Chilena de Química
publishDate	2012
url	http://www.scielo.cl/scielo.php?script=sci_arttext&pid=S0717-97072012000300020
work_keys_str_mv	AT pazcristian synthesisandacheinhibitingactivityof24substituted6phenylpyrimidines AT petermarting synthesisandacheinhibitingactivityof24substituted6phenylpyrimidines AT schmidtbernd synthesisandacheinhibitingactivityof24substituted6phenylpyrimidines AT becerrajose synthesisandacheinhibitingactivityof24substituted6phenylpyrimidines AT gutierrezmargarita synthesisandacheinhibitingactivityof24substituted6phenylpyrimidines AT astudilloluis synthesisandacheinhibitingactivityof24substituted6phenylpyrimidines AT silvamario synthesisandacheinhibitingactivityof24substituted6phenylpyrimidines
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SYNTHESIS AND AChE INHIBITING ACTIVITY OF 2, 4 SUBSTITUTED 6-PHENYL PYRIMIDINES

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