- COMPOUNDS
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A compound of formula (I), or a pharmaceutical salt thereof.
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Page/Page column 88
(2020/01/11)
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- USE OF A QUINAZOLINE COMPOUND IN PREPARING A MEDICAMENT AGAINST FLAVIVIRIDAE VIRUS
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Disclosed is a use of a quinazoline compound of Formula I having 2,4-diaminoquinazoline as a parent nucleus in preparation of a medicament for treating diseases caused by flaviviridae infection, especially a use in combating Hepatitis C virus infection and Dengue fever virus infection.
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Paragraph 0057-0058
(2013/10/08)
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- Discovery and optimization of 2,4-diaminoquinazoline derivatives as a new class of potent dengue virus inhibitors
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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 (EC50 = 0.15 μM). 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 (EC50 = 2.8 nM, SI > 1000) and an excellent pharmacokinetic profile.
- Chao, Bo,Tong, Xian-Kun,Tang, Wei,Li, De-Wen,He, Pei-Lan,Garcia, Jean-Michel,Zeng, Li-Min,Gao, An-Hui,Yang, Li,Li, Jia,Nan, Fa-Jun,Jacobs, Michael,Altmeyer, Ralf,Zuo, Jian-Ping,Hu, You-Hong
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experimental part
p. 3135 - 3143
(2012/06/01)
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- Direct Synthesis of 2,4-Diaminoquinazolines from 2-Fluorobenzonitriles
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In a search for new methods for preparing 2,4-diaminoquinazolines having a diversity of substituents in the benzenoid ring, it was found that the reaction of 2,6-difluorbenzonitrile with guanidine carbonate gave 2,4-diamino-5-fluoroquinazoline in excellent yield.Extension of this approach to other 2-fluorobenzonitriles, some of which were elaborated for the first time, showed that this reaction possesses considerable generality.The cyclization was sucessful even when electron donating groups were present at position six.Only in two cases where a primary or secondary amino group was also present ortho to the cyano group was this transformation unsucessful.
- Hynes, John B.,Pathak, Alpana,Panos, Constantina H.,Okeke, Claudia C.
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p. 1173 - 1177
(2007/10/02)
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