2019
DOI: 10.3390/molecules24050921
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Evolution and Biological Evaluation of Matrinic Derivatives with Amantadine Fragments As New Anti-Influenza Virus Agents

Abstract: A series of novel tricyclic matrinic derivatives with 11-adamantyl substitution were designed, synthesized, and evaluated for their activities against Influenza A H3N2 virus, based on the privileged structure strategy. Structure-activity relationship (SAR) analysis indicated that the introduction of an 11-adamantyl might be helpful for the potency. Among them, compounds 9f and 9j exhibited the promising anti-H3N2 activities with IC50 values of 7.2 μM and 10.2 μM, respectively, better than that of lead 1. Their… Show more

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Cited by 11 publications
(4 citation statements)
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“…The score ranged from zero, signifying no CPE, to four representing the most severe CPE for the inactivated virus’s CPE [ 18 ]. The most substantial alteration in CPE scoring is demonstrated in Figure-2 , primarily occurring on the 1 st day of the second passage.…”
Section: Resultsmentioning
confidence: 99%
See 1 more Smart Citation
“…The score ranged from zero, signifying no CPE, to four representing the most severe CPE for the inactivated virus’s CPE [ 18 ]. The most substantial alteration in CPE scoring is demonstrated in Figure-2 , primarily occurring on the 1 st day of the second passage.…”
Section: Resultsmentioning
confidence: 99%
“…Every day, the cells were checked for cytopathic and other effects. CPE severity levels were assessed on a scale from zero to four, where zero represented no observable CPE and four denoted 75%–100% observable CPE [ 18 ]. The third passage effectively inactivated the virus, as no CPE was detected at its end [ 19 ].…”
Section: Methodsmentioning
confidence: 99%
“…Second to the large superfamily of G-protein coupled receptors (GPCRs), ion channels are among the most soughtafter membrane-protein targets by the United States Federal Drug Administration. Ion-channel modulators in particular have shown therapeutic potential and successes, for example as blockers of influenza M2 channels (Moorthy et al, 2014;Sakai et al, 2018;Niu et al, 2019). It is expected that the current pandemic will prompt further research into this important area, with obvious therapeutic opportunities.…”
Section: Therapeutic Potential Of Channel Blockers Acting On Cov Ion mentioning
confidence: 99%
“…The insertion of norbornene and its derivatives into the organic molecules is creating a great impact in the field of medicinal and pharmaceutical chemistry . These types of insertion reactions are established with particular functional groups in the literature .…”
mentioning
confidence: 99%