Article

Design, synthesis and antiviral activity of novel pyridazines.

State Key Laboratory of Elemento-Organic Chemistry, Research Institute of Elemento-Organic Chemistry, Nankai University, 94 Weijing Street, Tianjin 300071, People's Republic of China.
European journal of medicinal chemistry (impact factor: 3.27). 04/2012; 54:33-41. DOI:10.1016/j.ejmech.2012.04.020 pp.33-41
Source: PubMed

ABSTRACT A series of pyridazines were prepared and evaluated for their anti-HIV activity. The new synthetic route involving a novel rearrangement reaction provided a practical method for the preparation of 5-hydroxypyridazines. The primary bioassay results indicated that most of the pyridazines possess anti-HIV activity. It ought to been mentioned that the rearranged compounds 35 and 39 exhibited relatively higher HIV inhibitory effect. Most of the synthesized compounds were also found to possess good anti-TMV activity, of which compound 9 showed similar in vivo anti-TMV activity to commercial plant virucide Ribavirin. This work provides a new and efficient approach to evolve novel multi-functional antiviral agents by rational integration and optimization of previously reported antiviral agents.

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Keywords

anti-HIV activity
 
antiviral agents
 
commercial plant virucide Ribavirin
 
compound 9
 
efficient approach
 
evolve novel multi-functional antiviral agents
 
good anti-TMV activity
 
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new synthetic route
 
practical method
 
rational integration
 
rearranged compounds 35
 
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synthesized compounds
 
vivo anti-TMV activity