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- Publisher Website: 10.1021/jm2015952
- Scopus: eid_2-s2.0-84859791780
- PMID: 22448770
- WOS: WOS:000302591100023
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Article: Discovery and Optimization of 2,4-Diaminoquinazoline Derivatives As a New Class of Potent Dengue Virus Inhibitors
Title | Discovery and Optimization of 2,4-Diaminoquinazoline Derivatives As a New Class of Potent Dengue Virus Inhibitors |
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Authors | |
Issue Date | 2012 |
Publisher | American 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 Identifier | http://hdl.handle.net/10722/164714 |
ISSN | 2023 Impact Factor: 6.8 2023 SCImago Journal Rankings: 1.986 |
ISI Accession Number ID |
DC Field | Value | Language |
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dc.contributor.author | Chao, B | en_US |
dc.contributor.author | Tong, XK | en_US |
dc.contributor.author | Tang, W | en_US |
dc.contributor.author | Li, DW | en_US |
dc.contributor.author | He, PL | en_US |
dc.contributor.author | Garcia, JM | en_US |
dc.contributor.author | Zeng, LM | en_US |
dc.contributor.author | Gao, AH | en_US |
dc.contributor.author | Yang, L | en_US |
dc.contributor.author | Li, J | en_US |
dc.contributor.author | Nan, FJ | en_US |
dc.contributor.author | Jacobs, M | en_US |
dc.contributor.author | Altmeyer, RM | en_US |
dc.contributor.author | Zuo, JP | en_US |
dc.contributor.author | Hu, YH | - |
dc.date.accessioned | 2012-09-20T08:08:31Z | - |
dc.date.available | 2012-09-20T08:08:31Z | - |
dc.date.issued | 2012 | en_US |
dc.identifier.citation | Journal of Medicinal Chemistry, 2012, v. 55 n. 7, p. 3135-3143 | en_US |
dc.identifier.issn | 0022-2623 | - |
dc.identifier.uri | http://hdl.handle.net/10722/164714 | - |
dc.description.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. | - |
dc.language | eng | en_US |
dc.publisher | American Chemical Society. The Journal's web site is located at http://pubs.acs.org/jmc | - |
dc.relation.ispartof | Journal of Medicinal Chemistry | en_US |
dc.subject.mesh | Antiviral Agents - chemical synthesis - pharmacokinetics - pharmacology | - |
dc.subject.mesh | Dengue Virus - drug effects - genetics | - |
dc.subject.mesh | Quinazolines - chemical synthesis - pharmacokinetics - pharmacology | - |
dc.subject.mesh | Replicon - drug effects | - |
dc.subject.mesh | Structure-Activity Relationship | - |
dc.title | Discovery and Optimization of 2,4-Diaminoquinazoline Derivatives As a New Class of Potent Dengue Virus Inhibitors | en_US |
dc.type | Article | en_US |
dc.identifier.email | Garcia, JM: jmgarcia@hku.hk | en_US |
dc.identifier.email | Altmeyer, RM: altmeyer@hkucc.hku.hk | - |
dc.identifier.doi | 10.1021/jm2015952 | - |
dc.identifier.pmid | 22448770 | - |
dc.identifier.scopus | eid_2-s2.0-84859791780 | - |
dc.identifier.hkuros | 205828 | en_US |
dc.identifier.volume | 55 | en_US |
dc.identifier.issue | 7 | - |
dc.identifier.spage | 3135 | en_US |
dc.identifier.epage | 3143 | en_US |
dc.identifier.isi | WOS:000302591100023 | - |
dc.publisher.place | United States | - |
dc.identifier.issnl | 0022-2623 | - |