Synthesis and Biological Evaluation of 2-oxo-pyrazine-3-carboxamide-yl Nucleoside Analogues and Their Epimers as Inhibitors of Influenza A Viruses

2014 ◽  
Vol 85 (3) ◽  
pp. 245-252 ◽  
Author(s):  
Jingjing Gao ◽  
Xianjin Luo ◽  
Yuhuan Li ◽  
Rongmei Gao ◽  
Haifeng Chen ◽  
...  
2003 ◽  
Vol 46 (26) ◽  
pp. 5763-5772 ◽  
Author(s):  
Svjetlana Prekupec ◽  
Draženka Svedružić ◽  
Tatjana Gazivoda ◽  
Draginja Mrvoš-Sermek ◽  
Ante Nagl ◽  
...  

ChemInform ◽  
2010 ◽  
Vol 32 (32) ◽  
pp. no-no
Author(s):  
Joern Wirsching ◽  
Juergen Voss ◽  
Gunadi Adiwidjaja ◽  
Jan Balzarini ◽  
Erik De Clercq

2002 ◽  
Vol 10 (2) ◽  
pp. 273-281 ◽  
Author(s):  
Cecilia H. Marzabadi ◽  
Richard W. Franck ◽  
Raymond F. Schinazi

2011 ◽  
Vol 19 (18) ◽  
pp. 5648-5669 ◽  
Author(s):  
K.C. Nicolaou ◽  
Shelby P. Ellery ◽  
Fatima Rivas ◽  
Karen Saye ◽  
Eric Rogers ◽  
...  

2014 ◽  
Vol 74 ◽  
pp. 388-397 ◽  
Author(s):  
Reham A.I. Abou-Elkhair ◽  
Ahmed H. Moustafa ◽  
Abdelfattah Z. Haikal ◽  
Ahmed M. Ibraheem

2005 ◽  
Vol 23 (12) ◽  
pp. 1659-1664 ◽  
Author(s):  
Da-Liang Li ◽  
Hong-Li Bao ◽  
Qi-Tao Tan ◽  
Yu-Ping Tan ◽  
Tian-Pa You

2014 ◽  
Vol 9 (7) ◽  
pp. 1934578X1400900
Author(s):  
Van Hung Nguyen ◽  
Van Cuong Pham ◽  
Thi Thao Do ◽  
Huong Doan Thi Mai ◽  
Nguyen Thanh Le ◽  
...  

New oseltamivir analogues were designed and synthesized, starting from shikimic acid. Biological evaluation against three human cancer cell lines (KB, MCF7 and Lu-1) showed that many of them exhibited cytotoxic activity. Azides 5 are more active than the corresponding amines 6. Thus, the reduction of the azide group into amine led to the loss of cytotoxicity. The compounds with a cyclohexanemethyloxy group at C-3 were more active than the other investigated compounds belonging to the same series. This cyclohexanemethyloxy group seems to be critical for the cytotoxic activity of this class of compounds. The synthetic oseltamivir analogues 6a-e had no inhibition activity, even at the concentration of 50 μM when they were evaluated for their in vitro influenza A neuraminidase inhibitory activity by an enzymatic assay.


2021 ◽  
Vol 22 (5) ◽  
pp. 2368
Author(s):  
Manu Kumar ◽  
Sang-Min Chung ◽  
Ganuskh Enkhtaivan ◽  
Rahul V. Patel ◽  
Han-Seung Shin ◽  
...  

In this study, we have introduced newly synthesized substituted benzothiazole based berberine derivatives that have been analyzed for their in vitro and in silico biological properties. The activity towards various kinds of influenza virus strains by employing the cytopathic effect (CPE) and sulforhodamine B (SRB) assay. Several berberine–benzothiazole derivatives (BBDs), such as BBD1, BBD3, BBD4, BBD5, BBD7, and BBD11, demonstrated interesting anti-influenza virus activity on influenza A viruses (A/PR/8/34, A/Vic/3/75) and influenza B viral (B/Lee/40, and B/Maryland/1/59) strain, respectively. Furthermore, by testing neuraminidase activity (NA) with the neuraminidase assay kit, it was identified that BBD7 has potent neuraminidase activity. The molecular docking analysis further suggests that the BBD1–BBD14 compounds’ antiviral activity may be because of interaction with residues of NA, and the same as in oseltamivir.


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