-transparent.png){kind=logo}
Synthesis and structure-activity relationships of novel arylpiperazines as potent antagonists of α1-adrenoceptor. 2016
Renata Oliveira Silva, and
Andressa Souza de Oliveira, and
Laís Flávia Nunes Lemes, and
Luciana de Camargo Nascente, and
Patrícia Coelho do Nascimento Nogueira, and
Edilberto R Silveira, and
Guilherme D Brand, and
Giulio Vistoli, and
Antonio Cilia, and
Elena Poggesi, and
Michela Buccioni, and
Gabriella Marucci, and
Maria Laura Bolognesi, and
Luiz Antonio Soares Romeiro
Department of Pharmacy, Health Sciences Faculty, University of Brasília, Campus Universitário Darcy Ribeiro, 70910-900, Brasília, DF, Brazil; LADETER, Catholic University of Brasília, QS 07, Lote 01, EPCT, Águas Claras, 71966-700, Brasília, DF, Brazil.
Arylpiperazines 2-11 were synthesized, and their biological profiles at α1-adrenergic receptors (α1-ARs) assessed by binding assays in CHO cells expressing human cloned subtypes and by functional experiments in isolated rat vas deferens (α1A), spleen (α1B), and aorta (α1D). Modifications at the 1,3-benzodioxole and phenyl phamacophoric units resulted in the identification of a number of potent compounds (moderately selective with respect to the α1b-AR), in binding experiments. Notably, compound 7 (LDT451) showed a subnanomolar pKi of 9.41 towards α1a-AR. An encouragingly lower α1B-potency was a general trend for all the series of compounds, which showed α1A/D over α1B selectivity in functional assays. If adequately optimized, such peculiar selectivity could have relevance for a potential LUTS/BPH therapeutic application.
Related Publications
Renata Oliveira Silva, and
Andressa Souza de Oliveira, and
Laís Flávia Nunes Lemes, and
Luciana de Camargo Nascente, and
Patrícia Coelho do Nascimento Nogueira, and
Edilberto R Silveira, and
Guilherme D Brand, and
Giulio Vistoli, and
Antonio Cilia, and
Elena Poggesi, and
Michela Buccioni, and
Gabriella Marucci, and
Maria Laura Bolognesi, and
Luiz Antonio Soares Romeiro
January 2004,
Journal of medicinal chemistry,
Renata Oliveira Silva, and
Andressa Souza de Oliveira, and
Laís Flávia Nunes Lemes, and
Luciana de Camargo Nascente, and
Patrícia Coelho do Nascimento Nogueira, and
Edilberto R Silveira, and
Guilherme D Brand, and
Giulio Vistoli, and
Antonio Cilia, and
Elena Poggesi, and
Michela Buccioni, and
Gabriella Marucci, and
Maria Laura Bolognesi, and
Luiz Antonio Soares Romeiro
June 2013,
Bioorganic & medicinal chemistry letters,
Renata Oliveira Silva, and
Andressa Souza de Oliveira, and
Laís Flávia Nunes Lemes, and
Luciana de Camargo Nascente, and
Patrícia Coelho do Nascimento Nogueira, and
Edilberto R Silveira, and
Guilherme D Brand, and
Giulio Vistoli, and
Antonio Cilia, and
Elena Poggesi, and
Michela Buccioni, and
Gabriella Marucci, and
Maria Laura Bolognesi, and
Luiz Antonio Soares Romeiro
February 2005,
Bioorganic & medicinal chemistry letters,
Renata Oliveira Silva, and
Andressa Souza de Oliveira, and
Laís Flávia Nunes Lemes, and
Luciana de Camargo Nascente, and
Patrícia Coelho do Nascimento Nogueira, and
Edilberto R Silveira, and
Guilherme D Brand, and
Giulio Vistoli, and
Antonio Cilia, and
Elena Poggesi, and
Michela Buccioni, and
Gabriella Marucci, and
Maria Laura Bolognesi, and
Luiz Antonio Soares Romeiro
August 2012,
Bioorganic & medicinal chemistry letters,
Renata Oliveira Silva, and
Andressa Souza de Oliveira, and
Laís Flávia Nunes Lemes, and
Luciana de Camargo Nascente, and
Patrícia Coelho do Nascimento Nogueira, and
Edilberto R Silveira, and
Guilherme D Brand, and
Giulio Vistoli, and
Antonio Cilia, and
Elena Poggesi, and
Michela Buccioni, and
Gabriella Marucci, and
Maria Laura Bolognesi, and
Luiz Antonio Soares Romeiro
July 2013,
Bioorganic & medicinal chemistry letters,
Renata Oliveira Silva, and
Andressa Souza de Oliveira, and
Laís Flávia Nunes Lemes, and
Luciana de Camargo Nascente, and
Patrícia Coelho do Nascimento Nogueira, and
Edilberto R Silveira, and
Guilherme D Brand, and
Giulio Vistoli, and
Antonio Cilia, and
Elena Poggesi, and
Michela Buccioni, and
Gabriella Marucci, and
Maria Laura Bolognesi, and
Luiz Antonio Soares Romeiro
November 2006,
Bioorganic & medicinal chemistry,
Renata Oliveira Silva, and
Andressa Souza de Oliveira, and
Laís Flávia Nunes Lemes, and
Luciana de Camargo Nascente, and
Patrícia Coelho do Nascimento Nogueira, and
Edilberto R Silveira, and
Guilherme D Brand, and
Giulio Vistoli, and
Antonio Cilia, and
Elena Poggesi, and
Michela Buccioni, and
Gabriella Marucci, and
Maria Laura Bolognesi, and
Luiz Antonio Soares Romeiro
August 2002,
Bioorganic & medicinal chemistry letters,
Renata Oliveira Silva, and
Andressa Souza de Oliveira, and
Laís Flávia Nunes Lemes, and
Luciana de Camargo Nascente, and
Patrícia Coelho do Nascimento Nogueira, and
Edilberto R Silveira, and
Guilherme D Brand, and
Giulio Vistoli, and
Antonio Cilia, and
Elena Poggesi, and
Michela Buccioni, and
Gabriella Marucci, and
Maria Laura Bolognesi, and
Luiz Antonio Soares Romeiro
August 2009,
Bioorganic & medicinal chemistry letters,
Renata Oliveira Silva, and
Andressa Souza de Oliveira, and
Laís Flávia Nunes Lemes, and
Luciana de Camargo Nascente, and
Patrícia Coelho do Nascimento Nogueira, and
Edilberto R Silveira, and
Guilherme D Brand, and
Giulio Vistoli, and
Antonio Cilia, and
Elena Poggesi, and
Michela Buccioni, and
Gabriella Marucci, and
Maria Laura Bolognesi, and
Luiz Antonio Soares Romeiro
August 2019,
Bioorganic & medicinal chemistry letters,
Renata Oliveira Silva, and
Andressa Souza de Oliveira, and
Laís Flávia Nunes Lemes, and
Luciana de Camargo Nascente, and
Patrícia Coelho do Nascimento Nogueira, and
Edilberto R Silveira, and
Guilherme D Brand, and
Giulio Vistoli, and
Antonio Cilia, and
Elena Poggesi, and
Michela Buccioni, and
Gabriella Marucci, and
Maria Laura Bolognesi, and
Luiz Antonio Soares Romeiro
December 1997,
Chemical & pharmaceutical bulletin,
