2011
DOI: 10.1016/j.bmcl.2011.08.002
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Synthesis, structure–activity relationship and in vitro biological evaluation of N-arylethyl isoquinoline derivatives as Coxsackievirus B3 inhibitors

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Cited by 14 publications
(4 citation statements)
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“…Compound 1 and its 16 diastereoisomers (Table 1, Groups A and B) and 16 regioisomers (Table 1, Groups C and D) were evaluated for their antiviral inhibitory activities against CVB3 in African green monkey kidney cells (Vero cells), which were infected with CVB3 and measured with CPE assay. 34 The preliminary biological study showed that compound 1 and its regioisomer 39 displayed the most potent activities against CVB3 among all the isomers, with IC 50 values of 2.1 mM and 3.7 mM and SI values of 5.2 and 4.3, respectively, which are better than those of the positive control ribavirin (IC 50 1577.5 mM and SI ¼ 5.2) but less effective than those of pleconaril. Diastereoisomer 23 and regioisomers 35, 37, 41, 42, and 47 also exhibited good inhibition against CVB3, with IC 50 values ranging from 8.6-11.1 mM.…”
Section: Antiviral Screening and Stereostructure-activity Relationshipmentioning
confidence: 95%
“…Compound 1 and its 16 diastereoisomers (Table 1, Groups A and B) and 16 regioisomers (Table 1, Groups C and D) were evaluated for their antiviral inhibitory activities against CVB3 in African green monkey kidney cells (Vero cells), which were infected with CVB3 and measured with CPE assay. 34 The preliminary biological study showed that compound 1 and its regioisomer 39 displayed the most potent activities against CVB3 among all the isomers, with IC 50 values of 2.1 mM and 3.7 mM and SI values of 5.2 and 4.3, respectively, which are better than those of the positive control ribavirin (IC 50 1577.5 mM and SI ¼ 5.2) but less effective than those of pleconaril. Diastereoisomer 23 and regioisomers 35, 37, 41, 42, and 47 also exhibited good inhibition against CVB3, with IC 50 values ranging from 8.6-11.1 mM.…”
Section: Antiviral Screening and Stereostructure-activity Relationshipmentioning
confidence: 95%
“…Antiviral assays against influenza virus A strains A/FM/1/47 (H1N1) and A/Hanfang/359/95 (H3N2) and coxsackie virus B3 were performed as described previously …”
Section: Experimental Sectionmentioning
confidence: 99%
“…Naturally occurring isoquinoline alkaloids have been an interesting structural class of compounds with potential medicinal and pharmacological applications . Isoquinolinium salts were also reported as cholinesterase inhibitors , antiviral agents , and leishmanicidal pharmacophores . In addition, the use of heteroaromatic N ‐ylides as 1,3‐dipoles is one of the most versatile synthetic tools for obtaining condensed heterocyclic structures via [3 + 2] cycloadditions .…”
Section: Introductionmentioning
confidence: 99%