- Discovery of Adamantane Carboxamides as Ebola Virus Cell Entry and Glycoprotein Inhibitors
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We identified and explored the structure-activity-relationship (SAR) of an adamantane carboxamide chemical series of Ebola virus (EBOV) inhibitors. Selected analogs exhibited half-maximal inhibitory concentrations (EC50 values) of ~10-15 nM in vesicular s
- Plewe, Michael B.,Sokolova, Nadezda V.,Gantla, Vidyasagar Reddy,Brown, Eric R.,Naik, Shibani,Fetsko, Alexandra,Lorimer, Donald D.,Lorimer, Donald D.,Dranow, David M.,Dranow, David M.,Smutney, Hayden,Smutney, Hayden,Bullen, Jameson,Bullen, Jameson,Sidhu, Rana,Sidhu, Rana,Master, Arshil,Master, Arshil,Wang, Junru,Wang, Junru,Kallel, E. Adam,Zhang, Lihong,Kalveram, Birte,Freiberg, Alexander N.,Henkel, Greg,McCormack, Ken
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supporting information
p. 1160 - 1167
(2020/05/14)
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- ADAMANTANE DERIVATIVES FOR THE TREATMENT OF FILOVIRUS INFECTION
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Compounds of structural Formula I were developed for the treatment of infections by filoviruses including Ebolavirus and Marburgvirus, wherein, R1, R2, R3, X and Y are defined in the specification.
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Paragraph 0898-0899; 0904-0905
(2020/02/05)
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- SPHINGOSINE KINASE INHIBITORS
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The invention relates to substituted adamantane compounds, pharmaceutical compositions thereof, processes for their preparation, and methods for inhibiting sphingosine kinase and for treating or preventing hyperproliferative disease, inflammatory disease, or angiogenic disease.
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Page/Page column 44
(2008/06/13)
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- Synthesis of 3-Aryl-1-adamantanemethylamines
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Friedel-Crafts alkylations of fluorobenzene, thioanisole, and thiophene with 3-bromo-1-adamantanecarboxylic acid are reported.Various Lewis acids (AlCl3, FeCl3, ZnCl2, SnCl4) served as effective catalysts for these substitution reactions.The products were 3-aryl-1-adamantanecarboxylic acids.Substitution took place in fluorobenzene and thioanisole at the para position and in thiophene at positions 2 and 3.These acids were reacted with phosphorus pentachloride and then ammonia to form amides which were reduced by lithium aluminum hydride to provide the corresponding3-aryl-1-adamantanemethylamines.
- Handa, Indra,Bauer, Ludwig
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p. 223 - 225
(2007/10/02)
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