55791-66-7Relevant academic research and scientific papers
Ortho -Substituted lipidated Brartemicin derivative shows promising Mincle-mediated adjuvant activity
Foster, Amy J.,Kodar, Kristel,Stocker, Bridget L.,Timmer, Mattie S. M.
supporting information, p. 1095 - 1103 (2020/02/22)
The macrophage inducible C-type lectin (Mincle) is a pathogen recognition receptor (PRR) that is a promising target for the development of Th1-polarising vaccine adjuvants. We recently reported on the synthesis and evaluation of lipidated Brartemicin analogues that showed Mincle agonist activity, with our lead agonist exhibiting potent Th1 adjuvant activity that was greater than that of trehalose dibehenate (TDB). Herein, we report on the efficient synthesis and subsequent biological evaluation of additional lipidated Brartemicin analogues that were designed to determine the structural requirements for optimal Mincle signalling. While all the Brartemicin analogues retained their ability to signal through Mincle and induce a functional response, the o-substituted and m,m-disubstituted derivatives (5a and 5d, respectively) induced a potent inflammatory response when using cells of both murine and human origin, with this response being the greatest observed thus far. As the inflammatory response elicited by 5a was slightly better than that induced by 5d, our findings point to o-substituted Brartemicin analogues as the preferred scaffold for further adjuvant development.
BRARTEMICIN ANALOGUES
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Page/Page column 34; 73, (2019/05/22)
The invention relates to brartemicin analogues of Formula (IV) and their uses. These compounds are potent Mincle agonists and Th1-stimulating vaccine adjuvants.
Potential antiatherosclerotic agents. 2. (Aralkylamino)- and (alkylamino)benzoic acid analogues of cetaben
Albright,DeVries,Largis,Miner,Reich,Schaffer,Shepherd,Upeslacis
, p. 1378 - 1393 (2007/10/02)
The syntheses of a series of (aralkylamino)- and (alkylamino)benzoic acids, as well as the corresponding esters and sodium salts, are described. The compounds were evaluated in vivo in rats for serum sterol and triglyceride lowering activity and in vitro
