The development of HIV-1 dual inhibitors is a highly innovative approach aimed at reducing drug toxic side effects as well as therapeutic costs. HIV-1 integrase (IN) and reverse transcriptase-associated ribonuclease H (RNase H) are both selective targets for HIV-1 chemotherapy, and the identification of dual IN/RNase H inhibitors is an attractive strategy for new drug development. We newly synthesized pyrrolyl derivatives that exhibited good potency against IN and a moderate inhibition of the RNase H function of RT, confirming the possibility of developing dual HIV-1 IN/RNase H inhibitors and obtaining new information for the further development of more effective dual HIV-1 inhibitors

Structure−activity relationship of pyrrolyl diketo acid derivatives as dual Inhibitors of HIV‑1 integrase and reverse transcriptase ribonuclease H domain / Cuzzucoli Crucitti, Giuliana; Métifiot, Mathieu; Pescatori, Luca; Messore, Antonella; Madia, VALENTINA NOEMI; Pupo, Giovanni; Saccoliti, Francesco; Scipione, Luigi; Tortorella, Silvano; Esposito, Francesca; Corona, Angela; Cadeddu, Marta; Marchand, Christophe; Pommier, Yves; Tramontano, Enzo; Costi, Roberta; DI SANTO, Roberto. - In: JOURNAL OF MEDICINAL CHEMISTRY. - ISSN 0022-2623. - STAMPA. - 58:4(2015), pp. 1915-1928. [10.1021/jm501799k]

Structure−activity relationship of pyrrolyl diketo acid derivatives as dual Inhibitors of HIV‑1 integrase and reverse transcriptase ribonuclease H domain

PESCATORI, LUCA;MESSORE, ANTONELLA;MADIA, VALENTINA NOEMI;PUPO, GIOVANNI;SACCOLITI, FRANCESCO;SCIPIONE, Luigi;TORTORELLA, Silvano;COSTI, Roberta
Penultimo
;
DI SANTO, Roberto
Ultimo
2015

Abstract

The development of HIV-1 dual inhibitors is a highly innovative approach aimed at reducing drug toxic side effects as well as therapeutic costs. HIV-1 integrase (IN) and reverse transcriptase-associated ribonuclease H (RNase H) are both selective targets for HIV-1 chemotherapy, and the identification of dual IN/RNase H inhibitors is an attractive strategy for new drug development. We newly synthesized pyrrolyl derivatives that exhibited good potency against IN and a moderate inhibition of the RNase H function of RT, confirming the possibility of developing dual HIV-1 IN/RNase H inhibitors and obtaining new information for the further development of more effective dual HIV-1 inhibitors
2015
dose-response relationship drug; HIV; HIV integrase; HIV integrase inhibitors; HIV reverse transcriptase; microbial sensitivity tests; molecular structure; protein structure tertiary; pyrroles; reverse transcriptase inhibitors; ribonuclease H; Structure-Activity Relationship; Virus Replication; Molecular Medicine; Drug Discovery3003 Pharmaceutical Science; Medicine (all)
01 Pubblicazione su rivista::01a Articolo in rivista
Structure−activity relationship of pyrrolyl diketo acid derivatives as dual Inhibitors of HIV‑1 integrase and reverse transcriptase ribonuclease H domain / Cuzzucoli Crucitti, Giuliana; Métifiot, Mathieu; Pescatori, Luca; Messore, Antonella; Madia, VALENTINA NOEMI; Pupo, Giovanni; Saccoliti, Francesco; Scipione, Luigi; Tortorella, Silvano; Esposito, Francesca; Corona, Angela; Cadeddu, Marta; Marchand, Christophe; Pommier, Yves; Tramontano, Enzo; Costi, Roberta; DI SANTO, Roberto. - In: JOURNAL OF MEDICINAL CHEMISTRY. - ISSN 0022-2623. - STAMPA. - 58:4(2015), pp. 1915-1928. [10.1021/jm501799k]
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Utilizza questo identificativo per citare o creare un link a questo documento: https://hdl.handle.net/11573/895359
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