Pyrrolyl Pyrazoles as Non-Diketo Acid Inhibitors of the HIV-1 Ribonuclease H Function of Reverse Transcriptase.


Journal

ACS medicinal chemistry letters
ISSN: 1948-5875
Titre abrégé: ACS Med Chem Lett
Pays: United States
ID NLM: 101521073

Informations de publication

Date de publication:
14 May 2020
Historique:
received: 19 12 2019
accepted: 05 03 2020
entrez: 22 5 2020
pubmed: 22 5 2020
medline: 22 5 2020
Statut: epublish

Résumé

Due to the biological liability of diketo acid (DKA) chain, we transferred this element of our previously reported anti-HIV-1 pyrrolyl derivatives to a non-DKA scaffold, obtaining a series of pyrrolyl-pyrazole carboxylic acids as new RNase H inhibitors. Among the newly synthesized derivatives, oxyphenylpyrrolyl-pyrazoles demonstrated inhibitory activities within the low micromolar/submicromolar range with compound

Identifiants

pubmed: 32435387
doi: 10.1021/acsmedchemlett.9b00617
pmc: PMC7236236
doi:

Types de publication

Journal Article

Langues

eng

Pagination

798-805

Informations de copyright

Copyright © 2020 American Chemical Society.

Déclaration de conflit d'intérêts

The authors declare no competing financial interest.

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Auteurs

Antonella Messore (A)

Dipartimento di Chimica e Tecnologie del Farmaco, Istituto Pasteur-Fondazione Cenci Bolognetti, "Sapienza" Università di Roma, p.le Aldo Moro 5, I-00185 Roma, Italy.

Angela Corona (A)

Department of Life and Environmental Sciences, University of Cagliari, Cittadella Universitaria di Monserrato, SS554-09042 Monserrato (CA), Italy.

Valentina Noemi Madia (VN)

Dipartimento di Chimica e Tecnologie del Farmaco, Istituto Pasteur-Fondazione Cenci Bolognetti, "Sapienza" Università di Roma, p.le Aldo Moro 5, I-00185 Roma, Italy.

Francesco Saccoliti (F)

Dipartimento di Chimica e Tecnologie del Farmaco, Istituto Pasteur-Fondazione Cenci Bolognetti, "Sapienza" Università di Roma, p.le Aldo Moro 5, I-00185 Roma, Italy.

Valeria Tudino (V)

Dipartimento di Chimica e Tecnologie del Farmaco, Istituto Pasteur-Fondazione Cenci Bolognetti, "Sapienza" Università di Roma, p.le Aldo Moro 5, I-00185 Roma, Italy.

Alessandro De Leo (A)

Dipartimento di Chimica e Tecnologie del Farmaco, Istituto Pasteur-Fondazione Cenci Bolognetti, "Sapienza" Università di Roma, p.le Aldo Moro 5, I-00185 Roma, Italy.

Luigi Scipione (L)

Dipartimento di Chimica e Tecnologie del Farmaco, Istituto Pasteur-Fondazione Cenci Bolognetti, "Sapienza" Università di Roma, p.le Aldo Moro 5, I-00185 Roma, Italy.

Daniela De Vita (D)

Dipartimento di Chimica e Tecnologie del Farmaco, Istituto Pasteur-Fondazione Cenci Bolognetti, "Sapienza" Università di Roma, p.le Aldo Moro 5, I-00185 Roma, Italy.

Giorgio Amendola (G)

DiSTABiF, University of Campania "Luigi Vanvitelli", Via Vivaldi 43, 81100 Caserta, Italy.

Salvatore Di Maro (S)

DiSTABiF, University of Campania "Luigi Vanvitelli", Via Vivaldi 43, 81100 Caserta, Italy.

Ettore Novellino (E)

Department of Pharmacy, University Federico II of Naples, Via D. Montesano 49, 80131 Naples, Italy.

Sandro Cosconati (S)

DiSTABiF, University of Campania "Luigi Vanvitelli", Via Vivaldi 43, 81100 Caserta, Italy.

Mathieu Métifiot (M)

Laboratoire MFP, UMR 5234, CNRS, Université de Bordeaux, 146 rue Léo Saignat, 33076 Bordeaux cedex, France.

Marie-Line Andreola (ML)

Laboratoire MFP, UMR 5234, CNRS, Université de Bordeaux, 146 rue Léo Saignat, 33076 Bordeaux cedex, France.

Piera Valenti (P)

Department of Public Health and Infectious Diseases, "Sapienza" University of Rome, p.le Aldo Moro 5, I-00185 Rome, Italy.

Francesca Esposito (F)

Department of Life and Environmental Sciences, University of Cagliari, Cittadella Universitaria di Monserrato, SS554-09042 Monserrato (CA), Italy.

Nicole Grandi (N)

Department of Life and Environmental Sciences, University of Cagliari, Cittadella Universitaria di Monserrato, SS554-09042 Monserrato (CA), Italy.

Enzo Tramontano (E)

Department of Life and Environmental Sciences, University of Cagliari, Cittadella Universitaria di Monserrato, SS554-09042 Monserrato (CA), Italy.

Roberta Costi (R)

Dipartimento di Chimica e Tecnologie del Farmaco, Istituto Pasteur-Fondazione Cenci Bolognetti, "Sapienza" Università di Roma, p.le Aldo Moro 5, I-00185 Roma, Italy.

Roberto Di Santo (R)

Dipartimento di Chimica e Tecnologie del Farmaco, Istituto Pasteur-Fondazione Cenci Bolognetti, "Sapienza" Università di Roma, p.le Aldo Moro 5, I-00185 Roma, Italy.

Classifications MeSH