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Article: Discovery and Optimization of 2,4-Diaminoquinazoline Derivatives As a New Class of Potent Dengue Virus Inhibitors

TitleDiscovery and Optimization of 2,4-Diaminoquinazoline Derivatives As a New Class of Potent Dengue Virus Inhibitors
Authors
Chao, BTong, XKTang, WLi, DWHe, PLGarcia, JMZeng, LMGao, AHYang, LLi, JNan, FJJacobs, MAltmeyer, RMZuo, JPHu, YH
Issue Date2012
PublisherAmerican Chemical Society. The Journal's web site is located at http://pubs.acs.org/jmc
Citation
Journal of Medicinal Chemistry, 2012, v. 55 n. 7, p. 3135-3143 How to Cite?
DOI: http://dx.doi.org/10.1021/jm2015952
AbstractThe results of a high-throughput screening assay using the DENV-2 replicon showed that the 2,4-diaminoquinazoline derivative 4a has a high dengue virus inhibitory activity (EC(50) = 0.15 muM). A series of 2,4-diaminoquinazoline derivatives based on 4a as a lead compound were synthesized and subjected to structure-antidengue activity relationship studies. Among the series of 2,4-diaminoquinazoline derivative probed, 4o was observed to display both the highest antiviral potency (EC(50) = 2.8 nM, SI > 1000) and an excellent pharmacokinetic profile.
Persistent Identifierhttp://hdl.handle.net/10722/164714
ISSN
0022-2623
2021 Impact Factor: 8.039
2020 SCImago Journal Rankings: 2.010
ISI Accession Number ID
WOS:000302591100023

 

DC FieldValueLanguage
dc.contributor.authorChao, Ben_US
dc.contributor.authorTong, XKen_US
dc.contributor.authorTang, Wen_US
dc.contributor.authorLi, DWen_US
dc.contributor.authorHe, PLen_US
dc.contributor.authorGarcia, JMen_US
dc.contributor.authorZeng, LMen_US
dc.contributor.authorGao, AHen_US
dc.contributor.authorYang, Len_US
dc.contributor.authorLi, Jen_US
dc.contributor.authorNan, FJen_US
dc.contributor.authorJacobs, Men_US
dc.contributor.authorAltmeyer, RMen_US
dc.contributor.authorZuo, JPen_US
dc.contributor.authorHu, YH-
dc.date.accessioned2012-09-20T08:08:31Z-
dc.date.available2012-09-20T08:08:31Z-
dc.date.issued2012en_US
dc.identifier.citationJournal of Medicinal Chemistry, 2012, v. 55 n. 7, p. 3135-3143en_US
dc.identifier.issn0022-2623-
dc.identifier.urihttp://hdl.handle.net/10722/164714-
dc.description.abstractThe results of a high-throughput screening assay using the DENV-2 replicon showed that the 2,4-diaminoquinazoline derivative 4a has a high dengue virus inhibitory activity (EC(50) = 0.15 muM). A series of 2,4-diaminoquinazoline derivatives based on 4a as a lead compound were synthesized and subjected to structure-antidengue activity relationship studies. Among the series of 2,4-diaminoquinazoline derivative probed, 4o was observed to display both the highest antiviral potency (EC(50) = 2.8 nM, SI > 1000) and an excellent pharmacokinetic profile.-
dc.languageengen_US
dc.publisherAmerican Chemical Society. The Journal's web site is located at http://pubs.acs.org/jmc-
dc.relation.ispartofJournal of Medicinal Chemistryen_US
dc.subject.meshAntiviral Agents - chemical synthesis - pharmacokinetics - pharmacology-
dc.subject.meshDengue Virus - drug effects - genetics-
dc.subject.meshQuinazolines - chemical synthesis - pharmacokinetics - pharmacology-
dc.subject.meshReplicon - drug effects-
dc.subject.meshStructure-Activity Relationship-
dc.titleDiscovery and Optimization of 2,4-Diaminoquinazoline Derivatives As a New Class of Potent Dengue Virus Inhibitorsen_US
dc.typeArticleen_US
dc.identifier.emailGarcia, JM: jmgarcia@hku.hken_US
dc.identifier.emailAltmeyer, RM: altmeyer@hkucc.hku.hk-
dc.identifier.doi10.1021/jm2015952-
dc.identifier.pmid22448770-
dc.identifier.scopuseid_2-s2.0-84859791780-
dc.identifier.hkuros205828en_US
dc.identifier.volume55en_US
dc.identifier.issue7-
dc.identifier.spage3135en_US
dc.identifier.epage3143en_US
dc.identifier.isiWOS:000302591100023-
dc.publisher.placeUnited States-
dc.identifier.issnl0022-2623-

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