Anti-HIV-1 activity of Pyrrol aryl sulfone (PAS) derivatives: synthesis and SAR studies of novel esters and amides at the position 2 of the pyrrole nucleus

Silvestri, R; Artico, M; La Regina, G; De Martino, G; La Colla, M; Loddo, Roberta; La Colla, P.

doi:10.1016/j.farmac.2003.11.004

A SAR study has been performed in order to evaluate how much the ester function could be a determinant for the anti-human immunodeficiency virus type-1 activity of pyrryl aryl sulfones (PASs), a potent family of non-nucleoside reverse transcriptase (RT) inhibitors discovered in the last years. Twenty-three new esters were prepared with the aim to enhance the inhibitory potency of 4a and 4c, two PAS agents endowed with good activity (EC50 = 0.14 microM) and deprived of cytotoxicity up to >200 microM. None of test derivatives was as potent as 4a and 4c and lacked of selectivity due to their higher cytotoxicity (compounds 22-25). Antiviral activity correlate with an ester ramified chain.

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Titolo:	Anti-HIV-1 activity of Pyrrol aryl sulfone (PAS) derivatives: synthesis and SAR studies of novel esters and amides at the position 2 of the pyrrole nucleus
Autori:	SILVESTRI R ARTICO M LA REGINA G DE MARTINO G LA COLLA M LODDO, ROBERTA LA COLLA P. mostra contributor esterni nascondi contributor esterni
Data di pubblicazione:	2004
Rivista:	IL FARMACO
Abstract:	A SAR study has been performed in order to evaluate how much the ester function could be a determinant for the anti-human immunodeficiency virus type-1 activity of pyrryl aryl sulfones (PASs), a potent family of non-nucleoside reverse transcriptase (RT) inhibitors discovered in the last years. Twenty-three new esters were prepared with the aim to enhance the inhibitory potency of 4a and 4c, two PAS agents endowed with good activity (EC50 = 0.14 microM) and deprived of cytotoxicity up to >200 microM. None of test derivatives was as potent as 4a and 4c and lacked of selectivity due to their higher cytotoxicity (compounds 22-25). Antiviral activity correlate with an ester ramified chain.
Handle:	http://hdl.handle.net/11584/13247
Tipologia:	1.1 Articolo in rivista

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