(3Z)-3-(2-[4-(aryl)-1,3-thiazol-2-yl]hydrazin-1-ylidene)-2,3-dihydro-1H-indol-2-one derivatives as dual inhibitors of HIV-1 reverse transcriptase.
Rita Meleddu
1
,
S. Distinto
1
,
A. W. Corona
2
,
Giulia Bianco
1
,
Valeria Cannas
1
,
Francesca Esposito
2
,
Anna Artese
3
,
Stefano Alcaro
3
,
Péter Mátyus
4
,
Dóra Bogdán
4
,
Filippo Cottiglia
1
,
Enzo Tramontano
2
,
E Maccioni
1
Publication type: Journal Article
Publication date: 2015-03-01
scimago Q1
wos Q1
SJR: 1.142
CiteScore: 11.3
Impact factor: 5.9
ISSN: 02235234, 17683254
PubMed ID:
25728026
Organic Chemistry
Drug Discovery
General Medicine
Pharmacology
Abstract
The HIV-1 Reverse Transcriptase (RT) is a validated and deeply explored biological target for the treatment of AIDS. However, only drugs targeting the RT-associated DNA polymerase (DP) function have been approved for clinical use. We designed and synthesised a new generation of HIV-1 RT inhibitors, based on the (3Z)-3-(2-[4-(aryl)-1,3-thiazol-2-yl]hydrazin-1-ylidene)-2,3-dihydro-1H-indol-2-one scaffold. These compounds are active towards both RT-associated functions, DNA polymerase and ribonuclease H. The structure, biological activity and mode of action of the new derivatives have been investigated. In particular, the nature of the aromatic group in the position 4 of the thiazole ring plays a key role in the modulation of the activity towards the two RT-associated functions.
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48
Total citations:
48
Citations from 2025:
3
(6.25%)
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GOST
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Meleddu R. et al. (3Z)-3-(2-[4-(aryl)-1,3-thiazol-2-yl]hydrazin-1-ylidene)-2,3-dihydro-1H-indol-2-one derivatives as dual inhibitors of HIV-1 reverse transcriptase. // European Journal of Medicinal Chemistry. 2015. Vol. 93. pp. 452-460.
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Meleddu R., Distinto S., Corona A. W., Bianco G., Cannas V., Esposito F., Artese A., Alcaro S., Mátyus P., Bogdán D., Cottiglia F., Tramontano E., Maccioni E. (3Z)-3-(2-[4-(aryl)-1,3-thiazol-2-yl]hydrazin-1-ylidene)-2,3-dihydro-1H-indol-2-one derivatives as dual inhibitors of HIV-1 reverse transcriptase. // European Journal of Medicinal Chemistry. 2015. Vol. 93. pp. 452-460.
Cite this
RIS
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TY - JOUR
DO - 10.1016/j.ejmech.2015.02.032
UR - https://doi.org/10.1016/j.ejmech.2015.02.032
TI - (3Z)-3-(2-[4-(aryl)-1,3-thiazol-2-yl]hydrazin-1-ylidene)-2,3-dihydro-1H-indol-2-one derivatives as dual inhibitors of HIV-1 reverse transcriptase.
T2 - European Journal of Medicinal Chemistry
AU - Meleddu, Rita
AU - Distinto, S.
AU - Corona, A. W.
AU - Bianco, Giulia
AU - Cannas, Valeria
AU - Esposito, Francesca
AU - Artese, Anna
AU - Alcaro, Stefano
AU - Mátyus, Péter
AU - Bogdán, Dóra
AU - Cottiglia, Filippo
AU - Tramontano, Enzo
AU - Maccioni, E
PY - 2015
DA - 2015/03/01
PB - Elsevier
SP - 452-460
VL - 93
PMID - 25728026
SN - 0223-5234
SN - 1768-3254
ER -
Cite this
BibTex (up to 50 authors)
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@article{2015_Meleddu,
author = {Rita Meleddu and S. Distinto and A. W. Corona and Giulia Bianco and Valeria Cannas and Francesca Esposito and Anna Artese and Stefano Alcaro and Péter Mátyus and Dóra Bogdán and Filippo Cottiglia and Enzo Tramontano and E Maccioni},
title = {(3Z)-3-(2-[4-(aryl)-1,3-thiazol-2-yl]hydrazin-1-ylidene)-2,3-dihydro-1H-indol-2-one derivatives as dual inhibitors of HIV-1 reverse transcriptase.},
journal = {European Journal of Medicinal Chemistry},
year = {2015},
volume = {93},
publisher = {Elsevier},
month = {mar},
url = {https://doi.org/10.1016/j.ejmech.2015.02.032},
pages = {452--460},
doi = {10.1016/j.ejmech.2015.02.032}
}