10.3389/fchem.2019.00214.s001
Nicoletta Desideri
Nicoletta
Desideri
Rossella Fioravanti
Rossella
Fioravanti
Luca Proietti Monaco
Luca Proietti
Monaco
Elena Maria Atzori
Elena Maria
Atzori
Antonio Carta
Antonio
Carta
Ilenia Delogu
Ilenia
Delogu
Gabriella Collu
Gabriella
Collu
Roberta Loddo
Roberta
Loddo
Data_Sheet_1_Design, Synthesis, Antiviral Evaluation, and SAR Studies of New 1-(Phenylsulfonyl)-1H-Pyrazol−4-yl-Methylaniline Derivatives.PDF
Frontiers
2019
1-(phenylsulfonyl)-1H-pyrazole derivatives
antiviral activity
anti-Flavivirus activity
BVDV
RSV
2019-04-09 05:58:11
Dataset
https://frontiersin.figshare.com/articles/dataset/Data_Sheet_1_Design_Synthesis_Antiviral_Evaluation_and_SAR_Studies_of_New_1-_Phenylsulfonyl_-1H-Pyrazol_4-yl-Methylaniline_Derivatives_PDF/7969283
<p>A series of N-((3-phenyl-1-(phenylsulfonyl)-1H-pyrazol-4-yl)methyl)anilines 7a-p and 8a-l, structurally related to previously synthesized and tested (N-(1,3-diphenyl-1H-pyrazol-4-yl)methyl)anilines (1a-v), were designed and synthesized. The new derivatives were evaluated in cell-based assays for their cytotoxicity and antiviral activity against a large panel of RNA and DNA viruses of public health significance. Generally, the tested compounds did not display cytotoxicity toward the cell lines used. The majority of derivatives 7a-p were able to interfered with YFV and RSV replication in the micromolar range showing a marked improvement in potency and selectivity with respect to the reference inhibitors 6-azauridine and ribavirin, respectively. The introduction of a p-methoxy substituent on the phenylsulfonyl group (compounds 8a-l) completely abolished the anti-RSV activity and reduced or eliminated the potency against YFV. On the contrary, several p-methoxy analogs were able to interfere with BVDV replication with a comparable (8b, 8c, 8g, and 8k) or better (8a and 8f) potency than the reference inhibitor, ribavirin. Compound 7e, selected for time of addition experiments on BHK-21 cell cultures infected with YFV, achieved the highest reduction of virus titer when added 2 h post infection and maintained up to 4 h post infection.</p>