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>