tetano
Editor, Senior Moderator
Chem Biol Drug Des. 2016 Apr 9. doi: 10.1111/cbdd.12769. [Epub ahead of print]
[h=1]Synthesis of Pyrazine-1,3-thiazine hybrid analogues as antiviral agent against HIV-1, influenza A (H1N1), enterovirus 71 (EV71) and coxsackievirus B3 (CVB3).[/h] Wu HM[SUP]1[/SUP], Zhou K[SUP]1[/SUP], Wu T[SUP]2[/SUP], Cao YG[SUP]3,[/SUP][SUP]4[/SUP].
[h=3]Author information[/h]
[h=3]Abstract[/h] A novel series of pyrazine-1,3-thiazine hybrid conjugates were synthesized in excellent yield. These derivatives were subsequently tested against human immunodeficiency virus (HIV-1), Hemagglutinin Type 1 and Neuraminidase Type 1 - 'Influenza' A (H1N1) virus, enterovirus 71 (EV71) and coxsackievirus B3. The effect of these conjugates on the key enzymes responsible for the progression of these viral infections was also illustrated via enzyme based assay, such as HIV-1 reverse transcriptase (RT) and neuraminidase; where entire tested molecule showed considerable inhibition. Particularly, among the tested derivatives, compound 3k was identified as most promising inhibitor of HIV-1 with 94% of inhibition (IC[SUB]50[/SUB] 3.26?0.2 μM). Moreover, the compound 3d was found to be the most potent analogue to inhibit the H1N1 virus with IC[SUB]50[/SUB] of 5.32?0.4 μM together with inhibition of the Neuraminidase enzyme (IC[SUB]50[/SUB] 11.24?1.1 μM). In regard of inhibitory activity against, Enterovirus 71 (EV71) and coxsackievirus B3 (CVB3), the tested derivative showed considerable inhibition of infection. Molecular docking studies were also performed for the most promising inhibitors with their corresponding target protein to exemplify the structural requirement for better inhibitory activity. The results of inhibitory assay showed that, designed molecules possess considerable inhibitory activity against the virus tested. This article is protected by copyright. All rights reserved.
This article is protected by copyright. All rights reserved.
[h=4]KEYWORDS:[/h] H1N1; HIV-1; Synthesis; antiviral activity; coxsackievirus B3; enterovirus 71 (EV71)
PMID: 27062664 [PubMed - as supplied by publisher]
[h=1]Synthesis of Pyrazine-1,3-thiazine hybrid analogues as antiviral agent against HIV-1, influenza A (H1N1), enterovirus 71 (EV71) and coxsackievirus B3 (CVB3).[/h] Wu HM[SUP]1[/SUP], Zhou K[SUP]1[/SUP], Wu T[SUP]2[/SUP], Cao YG[SUP]3,[/SUP][SUP]4[/SUP].
[h=3]Author information[/h]
[h=3]Abstract[/h] A novel series of pyrazine-1,3-thiazine hybrid conjugates were synthesized in excellent yield. These derivatives were subsequently tested against human immunodeficiency virus (HIV-1), Hemagglutinin Type 1 and Neuraminidase Type 1 - 'Influenza' A (H1N1) virus, enterovirus 71 (EV71) and coxsackievirus B3. The effect of these conjugates on the key enzymes responsible for the progression of these viral infections was also illustrated via enzyme based assay, such as HIV-1 reverse transcriptase (RT) and neuraminidase; where entire tested molecule showed considerable inhibition. Particularly, among the tested derivatives, compound 3k was identified as most promising inhibitor of HIV-1 with 94% of inhibition (IC[SUB]50[/SUB] 3.26?0.2 μM). Moreover, the compound 3d was found to be the most potent analogue to inhibit the H1N1 virus with IC[SUB]50[/SUB] of 5.32?0.4 μM together with inhibition of the Neuraminidase enzyme (IC[SUB]50[/SUB] 11.24?1.1 μM). In regard of inhibitory activity against, Enterovirus 71 (EV71) and coxsackievirus B3 (CVB3), the tested derivative showed considerable inhibition of infection. Molecular docking studies were also performed for the most promising inhibitors with their corresponding target protein to exemplify the structural requirement for better inhibitory activity. The results of inhibitory assay showed that, designed molecules possess considerable inhibitory activity against the virus tested. This article is protected by copyright. All rights reserved.
This article is protected by copyright. All rights reserved.
[h=4]KEYWORDS:[/h] H1N1; HIV-1; Synthesis; antiviral activity; coxsackievirus B3; enterovirus 71 (EV71)
PMID: 27062664 [PubMed - as supplied by publisher]