tetano
Editor, Senior Moderator
Future Med Chem. 2018 Apr 9. doi: 10.4155/fmc-2017-0217. [Epub ahead of print]
[h=1]Second-generation nitazoxanide derivatives: thiazolides are effective inhibitors of the influenza A virus.[/h] Stachulski AV[SUP]1[/SUP], Santoro MG[SUP]2[/SUP], Piacentini S[SUP]2[/SUP], Belardo G[SUP]2[/SUP], Frazia S[SUP]2[/SUP], Pidathala C[SUP]1[/SUP], Row EC[SUP]3,[/SUP][SUP]4[/SUP], Berry NG[SUP]1[/SUP], Iqbal M[SUP]3,[/SUP][SUP]5[/SUP], Allman SA[SUP]6,[/SUP][SUP]7[/SUP], Semple JE[SUP]8,[/SUP][SUP]9[/SUP], Eklov BM[SUP]10[/SUP], O'Neill PM[SUP]1[/SUP], Rossignol JF[SUP]11,[/SUP][SUP]12[/SUP].
[h=3]Author information[/h]
[h=3]Abstract[/h] [h=4]AIM:[/h] The only small molecule drugs currently available for treatment of influenza A virus (IAV) are M2 ion channel blockers and sialidase inhibitors. The prototype thiazolide, nitazoxanide, has successfully completed Phase III clinical trials against acute uncomplicated influenza.
[h=4]RESULTS:[/h] We report the activity of seventeen thiazolide analogs against A/PuertoRico/8/1934(H1N1), a laboratory-adapted strain of the H1N1 subtype of IAV, in a cell culture-based assay. A total of eight analogs showed IC[SUB]50[/SUB]s in the range of 0.14-5.0 μM. Additionally a quantitative structure-property relationship study showed high correlation between experimental and predicted activity based on a molecular descriptor set.
[h=4]CONCLUSION:[/h] A range of thiazolides show useful activity against an H1N1 strain of IAV. Further evaluation of these molecules as potential new small molecule therapies is justified.
[h=4]KEYWORDS:[/h] antiviral drugs; computational chemistry; drug discovery; molecular modeling
PMID: 29629834 DOI: 10.4155/fmc-2017-0217
[h=1]Second-generation nitazoxanide derivatives: thiazolides are effective inhibitors of the influenza A virus.[/h] Stachulski AV[SUP]1[/SUP], Santoro MG[SUP]2[/SUP], Piacentini S[SUP]2[/SUP], Belardo G[SUP]2[/SUP], Frazia S[SUP]2[/SUP], Pidathala C[SUP]1[/SUP], Row EC[SUP]3,[/SUP][SUP]4[/SUP], Berry NG[SUP]1[/SUP], Iqbal M[SUP]3,[/SUP][SUP]5[/SUP], Allman SA[SUP]6,[/SUP][SUP]7[/SUP], Semple JE[SUP]8,[/SUP][SUP]9[/SUP], Eklov BM[SUP]10[/SUP], O'Neill PM[SUP]1[/SUP], Rossignol JF[SUP]11,[/SUP][SUP]12[/SUP].
[h=3]Author information[/h]
[h=3]Abstract[/h] [h=4]AIM:[/h] The only small molecule drugs currently available for treatment of influenza A virus (IAV) are M2 ion channel blockers and sialidase inhibitors. The prototype thiazolide, nitazoxanide, has successfully completed Phase III clinical trials against acute uncomplicated influenza.
[h=4]RESULTS:[/h] We report the activity of seventeen thiazolide analogs against A/PuertoRico/8/1934(H1N1), a laboratory-adapted strain of the H1N1 subtype of IAV, in a cell culture-based assay. A total of eight analogs showed IC[SUB]50[/SUB]s in the range of 0.14-5.0 μM. Additionally a quantitative structure-property relationship study showed high correlation between experimental and predicted activity based on a molecular descriptor set.
[h=4]CONCLUSION:[/h] A range of thiazolides show useful activity against an H1N1 strain of IAV. Further evaluation of these molecules as potential new small molecule therapies is justified.
[h=4]KEYWORDS:[/h] antiviral drugs; computational chemistry; drug discovery; molecular modeling
PMID: 29629834 DOI: 10.4155/fmc-2017-0217