tetano
Editor, Senior Moderator
Medchemcomm. 2017 Mar 3;8(5):960-963. doi: 10.1039/c6md00657d. eCollection 2017 May 1.
[h=1]Synthesis and in vitro study of novel borneol derivatives as potent inhibitors of the influenza A virus.[/h] Sokolova AS[SUP]1,[/SUP][SUP]2[/SUP], Yarovaya OI[SUP]1,[/SUP][SUP]2[/SUP], Semenova MD[SUP]1[/SUP], Shtro AA[SUP]3[/SUP], Orshanskaya IR[SUP]3[/SUP], Zarubaev VV[SUP]3[/SUP], Salakhutdinov NF[SUP]1,[/SUP][SUP]2[/SUP].
[h=3]Author information[/h]
[h=3]Abstract[/h] Herein, we present the design and synthesis of a series of novel heterocyclic derivatives of (-)-borneol and (-)-isoborneol as potent inhibitors of the influenza A virus. All compounds were tested for their toxicity against MDCK cells and for virus-inhibiting activity against the influenza virus A/Puerto Rico/8/34 (H1N1). Compounds 7, 16 and 26 containing a morpholine fragment exhibited the highest efficiency as agents inhibiting the replication of the influenza virus A(H1N1) with selectivity indices of 82, 45 and 65, correspondingly. Derivatives 9 (SI = 23) and 18 (SI = 25) containing a 1-methylpiperazine motif showed moderate antiviral activity. Structure-activity analysis of this new series of borneol derivatives revealed that a 1,7,7-trimethylbicyclo[2.2.1]heptan scaffold is required for the antiviral activity.
PMID: 30108810 PMCID: PMC6072209 DOI: 10.1039/c6md00657d
[h=1]Synthesis and in vitro study of novel borneol derivatives as potent inhibitors of the influenza A virus.[/h] Sokolova AS[SUP]1,[/SUP][SUP]2[/SUP], Yarovaya OI[SUP]1,[/SUP][SUP]2[/SUP], Semenova MD[SUP]1[/SUP], Shtro AA[SUP]3[/SUP], Orshanskaya IR[SUP]3[/SUP], Zarubaev VV[SUP]3[/SUP], Salakhutdinov NF[SUP]1,[/SUP][SUP]2[/SUP].
[h=3]Author information[/h]
[h=3]Abstract[/h] Herein, we present the design and synthesis of a series of novel heterocyclic derivatives of (-)-borneol and (-)-isoborneol as potent inhibitors of the influenza A virus. All compounds were tested for their toxicity against MDCK cells and for virus-inhibiting activity against the influenza virus A/Puerto Rico/8/34 (H1N1). Compounds 7, 16 and 26 containing a morpholine fragment exhibited the highest efficiency as agents inhibiting the replication of the influenza virus A(H1N1) with selectivity indices of 82, 45 and 65, correspondingly. Derivatives 9 (SI = 23) and 18 (SI = 25) containing a 1-methylpiperazine motif showed moderate antiviral activity. Structure-activity analysis of this new series of borneol derivatives revealed that a 1,7,7-trimethylbicyclo[2.2.1]heptan scaffold is required for the antiviral activity.
PMID: 30108810 PMCID: PMC6072209 DOI: 10.1039/c6md00657d