Next Article in Journal
HBX-6, Standardized Cornus officinalis and Psoralea corylifolia L. Extracts, Suppresses Benign Prostate Hyperplasia by Attenuating E2F1 Activation
Next Article in Special Issue
Current Aspects of siRNA Bioconjugate for In Vitro and In Vivo Delivery
Previous Article in Journal
Al(Salen) Metal Complexes in Stereoselective Catalysis
Article Menu
Issue 9 (May-1) cover image

Export Article

Open AccessFeature PaperArticle

Pyrimidine 2,4-Diones in the Design of New HIV RT Inhibitors

1
Dipartimento di Scienze Chimiche, Biologiche, Farmaceutiche ed Ambientali, Università di Messina, Via S.S. Annunziata, 98168 Messina, Italy
2
Dipartimento di Ingegneria, Università di Messina, Contrada Di Dio, 98166 Messina, Italy
3
Dipartimento di Chimica e Tecnologie Chimiche, Università della Calabria, Via P. Bucci 12/C, 87036 Arcavacata di Rende, Italy
4
Dipartimento di Scienze e Tecnologie Chimiche, Università di Roma “Tor Vergata”, 00133 Roma, Italy
5
IRCCS Centro Neurolesi “Bonino-Pulejo”, 98124 Messina, Italy
*
Authors to whom correspondence should be addressed.
Academic Editor: Erik De Clercq
Molecules 2019, 24(9), 1718; https://doi.org/10.3390/molecules24091718
Received: 18 February 2019 / Revised: 18 March 2019 / Accepted: 30 April 2019 / Published: 2 May 2019
  |  
PDF [2387 KB, uploaded 6 May 2019]
  |  

Abstract

The pyrimidine nucleus is a versatile core in the development of antiretroviral agents. On this basis, a series of pyrimidine-2,4-diones linked to an isoxazolidine nucleus have been synthesized and tested as nucleoside analogs, endowed with potential anti-HIV (human immunodeficiency virus) activity. Compounds 6ac, characterized by the presence of an ethereal group at C-3, show HIV reverse transcriptase (RT) inhibitor activity in the nanomolar range as well as HIV-infection inhibitor activity in the low micromolar with no toxicity. In the same context, compound 7b shows only a negligible inhibition of RT HIV. View Full-Text
Keywords: reverse nucleosides; Pyrimidine-2,4-dione derivatives; HIV RT inhibitors; biological activity; molecular docking reverse nucleosides; Pyrimidine-2,4-dione derivatives; HIV RT inhibitors; biological activity; molecular docking
Figures

Graphical abstract

This is an open access article distributed under the Creative Commons Attribution License which permits unrestricted use, distribution, and reproduction in any medium, provided the original work is properly cited (CC BY 4.0).

Supplementary material

SciFeed

Share & Cite This Article

MDPI and ACS Style

Romeo, R.; Iannazzo, D.; Veltri, L.; Gabriele, B.; Macchi, B.; Frezza, C.; Marino-Merlo, F.; Giofrè, S.V. Pyrimidine 2,4-Diones in the Design of New HIV RT Inhibitors. Molecules 2019, 24, 1718.

Show more citation formats Show less citations formats

Note that from the first issue of 2016, MDPI journals use article numbers instead of page numbers. See further details here.

Related Articles

Article Metrics

Article Access Statistics

1

Comments

[Return to top]
Molecules EISSN 1420-3049 Published by MDPI AG, Basel, Switzerland RSS E-Mail Table of Contents Alert
Back to Top