102408-31-1Relevant articles and documents
Human toll-like receptor 8-selective agonistic activities in 1-alkyl-1 h -benzimidazol-2-amines
Beesu, Mallesh,Malladi, Subbalakshmi S.,Fox, Lauren M.,Jones, Cassandra D.,Dixit, Anshuman,David, Sunil A.
, p. 7325 - 7341 (2014)
Toll-like receptor (TLR)-8 agonists strongly induce the production of T helper 1-polarizing cytokines and may therefore serve as promising candidate vaccine adjuvants, especially for the very young and the elderly. Earlier structure-based ligand design led to the identification of 3-pentyl-quinoline-2-amine as a novel, human TLR8-specific agonist. Comprehensive structure-activity relationships in ring-contracted 1-alkyl-1H-benzimidazol-2-amines were undertaken, and the best-in-class compound, 4-methyl-1-pentyl-1H-benzo[d]imidazol-2-amine, was found to be a pure TLR8 agonist, evoking strong proinflammatory cytokine and Type II interferon responses in human PBMCs, with no attendant CD69 upregulation in natural lymphocytic subsets. The 1-alkyl-1H-benzimidazol-2-amines represent a novel, alternate chemotype with pure TLR8-agonistic activities and will likely prove useful not only in understanding TLR8 signaling but also perhaps as a candidate vaccine adjuvant.
C3v-symmetric anion receptors with guanidine recognition motifs for ratiometric sensing of fluoride
Kim, Won,Sahoo, Suban K.,Kim, Gi-Dong,Choi, Heung-Jin
, p. 7872 - 7878 (2016/02/05)
Two new tripodal receptors 3 and 4 derived from a trindane framework having guanidine groups acting as hydrogen bond acceptors are synthesized and characterized for the selective recognition of anions. The anion recognition ability of the receptors was ev
TOLL-LIKE RECEPTOR AGONISTS
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Page/Page column 57; 58, (2015/02/25)
Compounds described herein can be used for therapeutic purposes. The compounds can be TLR agonists, such as TLR7 or TLR8 agonists. The compounds can be included in pharmaceutical compositions and used for therapies were being a TLR agonist is useful. The pharmaceutical compositions can include any ingredients, such as carries, diluents, excipients, fillers or the like that are common in pharmaceutical compositions. The compounds can be those illustrated or described herein as well as derivatives thereof, prodrugs thereof, salts thereof, or stereoisomers thereof, or having any chirality at any chiral center, or tautomer, polymorph, solvate, or combinations thereof. As such, the compounds can be used as adjuvants in vaccines, as well as for other therapeutic purposes described herein.
Inhibition and Dispersion of Bacterial Biofilms with 2-Aminobenzimidazole Derivatives
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Paragraph 0216; 0217; 0240; 0241, (2013/06/05)
Compounds described herein inhibit biofilm formation or disperse pre-formed biofilms of Gram-negative bacteria. Biofilm-inhibitory compounds can be encapsulated or contained in a polymer matrix for controlled release. Coatings, films, multilayer films, hydrogels, microspheres and nanospheres as well as pharmaceutical compositions and disinfecting compositions containing biofilm-inhibitory compounds are also provided. Methods for inhibiting formation of biofilms or dispersing already formed biofilms are provided. Methods for treating infections of gram-negative bacteria which form biofilms, particularly those of Pseudomonas and more particularly P. aeruginosa.
2-aminobenzimidazole derivatives strongly inhibit and disperse Pseudomonas aeruginosa biofilms
Frei, Reto,Breitbach, Anthony S.,Blackwell, Helen E.
supporting information; experimental part, p. 5226 - 5229 (2012/07/03)
Bacterial biofilms are exceptionally difficult to clear using traditional antibiotics and constitute a significant health threat. 2-Aminobenzimidazole derivatives (see scheme) are capable of strongly inhibiting the growth of and dispersing Pseudomonas aeruginosa biofilms. These molecules were found to modulate quorum sensing in reporter strains, and represent some of strongest P. aeruginosa biofilm inhibitors known. Copyright