613233-76-4Relevant academic research and scientific papers
Discovery and Structure-Activity Relationships of the Neoseptins: A New Class of Toll-like Receptor-4 (TLR4) Agonists
Morin, Matthew D.,Wang, Ying,Jones, Brian T.,Su, Lijing,Surakattula, Murali M. R. P.,Berger, Michael,Huang, Hua,Beutler, Elliot K.,Zhang, Hong,Beutler, Bruce,Boger, Dale L.
supporting information, p. 4812 - 4830 (2016/06/13)
Herein, we report studies leading to the discovery of the neoseptins and a comprehensive examination of the structure-activity relationships (SARs) of this new class of small-molecule mouse Toll-like receptor 4 (mTLR4) agonists. The compounds in this class, which emerged from screening an α-helix mimetic library, stimulate the immune response, act by a well-defined mechanism (mouse TLR4 agonist), are easy to produce and structurally manipulate, exhibit exquisite SARs, are nontoxic, and elicit improved and qualitatively different responses compared to lipopolysaccharide, even though they share the same receptor.
NEOSEPTINS: SMALL MOLECULE ADJUVANTS
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Page/Page column 124-125, (2014/09/03)
A MD-2:TLR4 complex agonist compound is disclosed whose structure corresponds to Formula (I), as defined within. Also disclosed are a method of its preparation and use, as well as a pharmaceutical composition containing the same.
Structure-activity relationships of the antimalarial agent artemisinin. 8. Design, synthesis, and CoMFA studies toward the development of artemisinin-based drugs against leishmaniasis and malaria
Avery, Mitchell A.,Muraleedharan, Kannoth M.,Desai, Prashant V.,Bandyopadhyaya, Achintya K.,Furtado, Marise M.,Tekwani, Babu L.
, p. 4244 - 4258 (2007/10/03)
Artemisinin (1) and its analogues have been well studied for their antimalarial activity. Here we present the antimalarial activity of some novel C-9-modified artemisinin analogues synthesized using artemisitene as the key intermediate. Further, antileish
ARTEMISININ-BASED PEROXIDE COMPOUNDS AS BROAD SPECTRUM ANTI-INFECTIVE AGENTS
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Page/Page column 22-23; 58-59, (2010/02/07)
Described herein is the synthesis, bioassay results and utility of new C-9 and C-10 substituted artemisinin derivatives with easily functionalizable groups attached to the artemisinin skeleton through carbon chain or heteroatoms. Described also is the demonstration of this class of compounds for their broad-spectrum anti-parasitic activity. Certain of these analogs possess noticeable cytotoxicity deliberately focused on treatment of cancerous diseases.
