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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
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?
Abstract
The 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
2013 Impact Factor: 5.480
2013 SCImago Journal Rankings: 2.348
ISI Accession Number ID

 

Author Affiliations
  1. Shanghai Institute of Materia Medica, Chinese Academy of Sciences
  2. HKU-Pasteur Research Centre
  3. UCL Medical School
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-

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