@article{6533bb9441bc4c238bebcfe91042a831,
title = "Development of triazoles and triazolium salts based on azt and their anti-viral activity against hiv-1",
abstract = "We report herein a set of 3′-azido-3′-deoxythymidine (AZT) derivatives based on triazoles and triazolium salts for HIV-1 infection. The compounds were synthesized via click chemistry with Cu(I) and Ru(II) catalysts. Triazolium salts were synthesized by reaction with methyl iodide or methyl triflate in good yields. The antiviral activity of the compounds was tested using two methodologies: In method one the activity was measured on infected cells; in method two a pre-exposure prophylaxis experimental model was employed. For method one the activity of the compounds was moderate, and in general the triazolium salts showed a decreased activity in relation to their triazole precursors. With method two the antiviral activity was higher. All compounds were able to decrease the infection, with two compounds able to clear almost all the infection, while a lower antiviral activity was noted for the triazolium salts. These results suggest that these drugs could play an important role in the development of pre-exposure prophylaxis therapies.",
keywords = "Anti-viral, AZT, Click chemistry, HIV-1, Triazoles, Triazolium salts",
author = "{de Alencar}, {Daniel Machado} and Juliana Gon{\c c}alves and Andreia Vieira and Cerqueira, {Sofia A.} and Cruz Sebasti{\~a}o and Leit{\~a}o, {Maria In{\^e}s P.S.} and Giulia Francescato and Paola Antenori and Helena Soares and Ana Petronilho",
note = "Funding Information: This research was funded by national funds through FCT?Funda??o para a Ci?ncia e a Tecnologia, I.P., Project MOSTMICRO-ITQB (refs. UIDB/04612/2020 and UIDP/04612/2020) to AP and IF/00109/2014/CP1244/CT0007 to AP, by IF/01722/2013 and CEECIND/01049/2020 to HS and by NovaSaude to AP and HS, Gilead G?nese PGG 009/2017 to HS and European Society of Clinical Microbiology and Infectious Diseases (ESCMID) to SC. JG, CS, SAC, MIPSL and GF were supported by FCT fellowships PD/BD/128343/2017, SFRH/BD/135296/2017, SFRH/BPD/124739/2016, PD/BD/135483/2018 and SFRH/BD/1444412019, respectively. Funding Information: Acknowledgments: The NMR spectra were acquired at CERMAX—ITQB, integrated in the National NMR Network and are partially supported by Infrastructure Project No. 022161 (co-financed by FEDER through COMPETE 2020, POCI, PORL and FCT through PIDDAC). Mass spectroscopy measurements were obtained by the UniMass Laboratory at ITQB-NOVA, Portugal. We thank Claudia Andrade for flow cytometry technical support. Funding Information: Funding: This research was funded by national funds through FCT—Funda{\c c}{\~a}o para a Ci{\^e}ncia e a Tecnologia, I.P., Project MOSTMICRO-ITQB (refs. UIDB/04612/2020 and UIDP/04612/2020) to AP and IF/00109/2014/CP1244/CT0007 to AP, by IF/01722/2013 and CEECIND/01049/2020 to HS and by NovaSaude to AP and HS, Gilead G{\'e}nese PGG 009/2017 to HS and European Society of Clinical Microbiology and Infectious Diseases (ESCMID) to SC. JG, CS, SAC, MIPSL and GF were supported by FCT fellowships PD/BD/128343/2017, SFRH/BD/135296/2017, SFRH/BPD/124739/2016, PD/BD/135483/2018 and SFRH/BD/1444412019, respectively. Publisher Copyright: {\textcopyright} 2021 by the authors. Licensee MDPI, Basel, Switzerland.",
year = "2021",
month = nov,
day = "1",
doi = "10.3390/molecules26216720",
language = "English",
volume = "26",
journal = "Molecules",
issn = "1420-3049",
publisher = "MDPI - Multidisciplinary Digital Publishing Institute",
number = "21",
}