1190215-03-2Relevant academic research and scientific papers
INHIBITORS TARGETING DRUG-RESISTANT INFLUENZA A
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Paragraph 0106; 0121, (2013/06/27)
Provided are compounds according to formula (la) or (lb) as described herein, that are capable of modulating the activity of influenza viruses (e.g., influenza A virus), for example, via interaction with the M2 transmembrane protein, and other similar viroporins. Also provided are methods for treating an influenza A-affected disease state or infection comprising administering a composition comprising one or more compounds according to according to formulas (la') or (lb), as described herein.
Heterodimers of histidine and amantadine as inhibitors for wild type and mutant M2 channels of influenza A
Zhang, Wenjuan,Xu, Jing,Liu, Fang,Li, Chufang,Jie, Yanling,Chen, Shaopeng,Li, Zhiyuan,Liu, Jinsong,Chen, Ling,Zhou, Guochun
experimental part, p. 1417 - 1423 (2011/01/04)
Inhibitors bearing the imidazole, adamantane and related structures were synthesized and tested against WT, S31N and S31N-L26I mutant M2 channels. Although amantadine (1) only inhibited WT M2 channel, compound 6 containing the imidazole and adamantane groups showed good inhibitory activity to WT and mutant M2 channels. The stereochemistry and basic pK a of α-amine are important for the activity of inhibitors and our data showed that derivatives of natural histidine are more active for M2 channels than those of unnatural histidine. The significance of our present results is that we have established a prospective strategy of drug discovery of WT and mutant M2 channels against influenza A.
