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.
Anti-HIV-1 Activity of Pyrryl Aryl Sulfone (PAS) Derivatives: Synthesis and SAR Studies of Novel Esters and Amides at the Position 2 of the Pyrrole Nucleus / Silvestri, Romano; Artico, Marino; LA REGINA, Giuseppe; DE MARTINO, G.; LA COLLA, M.; Loddo, R.; LA COLLA, P.. - In: IL FARMACO. - ISSN 0014-827X. - 59:(2004), pp. 201-210. [10.1016/j.farmac.2003.11.004]
Anti-HIV-1 Activity of Pyrryl Aryl Sulfone (PAS) Derivatives: Synthesis and SAR Studies of Novel Esters and Amides at the Position 2 of the Pyrrole Nucleus.
SILVESTRI, Romano;ARTICO, Marino;LA REGINA, GIUSEPPE;
2004
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.I documenti in IRIS sono protetti da copyright e tutti i diritti sono riservati, salvo diversa indicazione.
