Regioselective Synthesis of Pyrazolyl-pyrimidine Hybrids of Pharmacological Interest

Adriano F. Camargo; Mário A. Marangoni; Paulo A. de Moraes; Pablo A. Nogara; Blessing A. Afolabi; Carlos E. Bencke; João B. T. Rocha; Helio G. Bonacorso; Marcos A. P. Martins; Nilo Zanatta

doi:10.1055/s-0040-1707948

Synthesis, Inhaltsverzeichnis

Synthesis 2020; 52(16): 2347-2356
DOI: 10.1055/s-0040-1707948

paper

Regioselective Synthesis of Pyrazolyl-pyrimidine Hybrids of Pharmacological Interest

Adriano F. Camargo

^aNúcleo de Química de Heterociclos (NUQUIMHE), Departamento de Química, Universidade Federal de Santa Maria, 97105-900, Santa Maria, RS, Brazil eMail: nilo.zanatta@ufsm.br

,

Mário A. Marangoni

^aNúcleo de Química de Heterociclos (NUQUIMHE), Departamento de Química, Universidade Federal de Santa Maria, 97105-900, Santa Maria, RS, Brazil eMail: nilo.zanatta@ufsm.br

,

Paulo A. de Moraes

^aNúcleo de Química de Heterociclos (NUQUIMHE), Departamento de Química, Universidade Federal de Santa Maria, 97105-900, Santa Maria, RS, Brazil eMail: nilo.zanatta@ufsm.br

,

Pablo A. Nogara

^bDepartamento de Bioquímica e Biologia Molecular, Centro de Ciências Naturais e Exatas (CCNE), Universidade Federal de Santa Maria, 97105-900 Santa Maria, RS, Brazil

,

Blessing A. Afolabi

^bDepartamento de Bioquímica e Biologia Molecular, Centro de Ciências Naturais e Exatas (CCNE), Universidade Federal de Santa Maria, 97105-900 Santa Maria, RS, Brazil

,

Carlos E. Bencke

^aNúcleo de Química de Heterociclos (NUQUIMHE), Departamento de Química, Universidade Federal de Santa Maria, 97105-900, Santa Maria, RS, Brazil eMail: nilo.zanatta@ufsm.br

,

João B. T. Rocha

^bDepartamento de Bioquímica e Biologia Molecular, Centro de Ciências Naturais e Exatas (CCNE), Universidade Federal de Santa Maria, 97105-900 Santa Maria, RS, Brazil

,

Helio G. Bonacorso

^aNúcleo de Química de Heterociclos (NUQUIMHE), Departamento de Química, Universidade Federal de Santa Maria, 97105-900, Santa Maria, RS, Brazil eMail: nilo.zanatta@ufsm.br

,

Marcos A. P. Martins

^aNúcleo de Química de Heterociclos (NUQUIMHE), Departamento de Química, Universidade Federal de Santa Maria, 97105-900, Santa Maria, RS, Brazil eMail: nilo.zanatta@ufsm.br

,

Nilo Zanatta ∗

^aNúcleo de Química de Heterociclos (NUQUIMHE), Departamento de Química, Universidade Federal de Santa Maria, 97105-900, Santa Maria, RS, Brazil eMail: nilo.zanatta@ufsm.br

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Abstract

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Abstract

The regioselective synthesis of twenty novel [3-substituted 5-hydroxy-5-(trifluoromethyl)-4,5-dihydro-1H-pyrazol-1-yl][6-aryl-(2-methylthio)pyrimidin-4-yl]methanones from the cyclocondensation reactions of new 6-aryl-2-(methylthio)pyrimidine-4-carbohydrazides with 4-substituted 1,1,1-trifluorobut-3-en-2-ones is reported. Human acetylcholinesterase (HsAChE) and butyrylcholinesterase (HsBChE) inhibition tests were performed on selected products in order to explore the possible pharmacological applications of these compounds. Two compounds showed significant and selective inhibitory activity for BChE.

Key words

pyrazoles - pyrimidines - pyrazolyl-pyrimidines - BChE activity - trifluoromethyl enones

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Referenzen

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