Synthesis and anti-norovirus activity of pyranobenzopyrone compounds

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Show simple item record Pokhrel, Laxman Kim, Yunjeong Nguyen, Thi D.T. Prior, Allan M. Lu, Jianyu Chang, Kyeong-Ok Hua, Duy H. 2012-06-18T18:49:34Z 2012-06-18T18:49:34Z 2012-06-18
dc.description.abstract During the last decade, noroviruses have gained media attention as the cause of large scale outbreaks of gastroenteritis on cruise ships, dormitories, nursing homes, etc. Although noroviruses do not multiply in food or water, they can cause large outbreaks because approximately 10–100 virions are sufficient to cause illness in a healthy adult. Recently, it was shown that the activity of acyl-coenzyme A:cholesterol acyltransferase-1 (ACAT1) enzyme may be important in norovirus infection. In search of anti-noroviral agents based on the inhibition of ACAT1, we synthesized and evaluated the inhibitory activities of a class of pyranobenzopyrone molecules containing amino, pyridine, substituted quinolines, or 7,8-benzoquinoline nucleus. Three of the sixteen evaluated compounds possess ED[subscript]5[subscript]0 values in the low micrometer range. 2-Quinolylmethyl derivative 3A and 4-quinolylmethyl derivative 4A showed ED[subscript]5[subscript]0 values of 3.4 and 2.4 [mu]M and TD[subscript]5[subscript]0 values of >200 and 96.4 [mu]M, respectively. The identified active compounds are suitable for further modification for the development of anti-norovirus agents. en_US
dc.relation.uri en_US
dc.subject Acyl-coenzyme A:cholesterol en_US
dc.subject Acyltransferase (ACAT) en_US
dc.subject Caliciviruses en_US
dc.subject Norovirus en_US
dc.subject Anti-noroviruses en_US
dc.subject Pyranobenzopyrones en_US
dc.title Synthesis and anti-norovirus activity of pyranobenzopyrone compounds en_US
dc.type Article (author version) en_US 2012 en_US
dc.citation.doi doi: org/10.1016/j.bmcl.2012.03.084 en_US
dc.citation.epage 3484 en_US
dc.citation.issue 10 en_US
dc.citation.jtitle Bioorganic & Medicinal Chemistry Letters en_US
dc.citation.spage 3480 en_US
dc.citation.volume 22 en_US
dc.contributor.authoreid duy en_US
dc.contributor.authoreid lpokhrel en_US
dc.contributor.authoreid ykim en_US
dc.contributor.authoreid allanp en_US
dc.contributor.authoreid jianyulu en_US
dc.contributor.authoreid kchang en_US

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