64965-48-6Relevant articles and documents
AZABICYCLIC(THIO)AMIDES AS FUNGICIDAL COMPOUNDS
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Page/Page column 142, (2021/11/26)
The present invention relates to azabicyclic (thio)amide compounds and the uses thereof for controlling phytopathogenic microorganisms such as phytopathogenic fungi. It also relates to processes and intermediates for preparing these compounds
Exquisite selectivity for human toll-like receptor 8 in substituted furo[2,3-c]quinolines
Kokatla, Hari Prasad,Sil, Diptesh,Malladi, Subbalakshmi S.,Balakrishna, Rajalakshmi,Hermanson, Alec R.,Fox, Lauren M.,Wang, Xinkun,Dixit, Anshuman,David, Sunil A.
, p. 6871 - 6885 (2013/10/01)
Toll-like receptor (TLR)-8 agonists activate adaptive immune responses by inducing robust production of T helper 1-polarizing cytokines, suggesting that TLR8-active compounds may be promising candidate adjuvants. We synthesized and evaluated hitherto unexplored furo[2,3-c]quinolines and regioisomeric furo[3,2-c]quinolines derived via a tandem, one-pot Sonogashira coupling and intramolecular 5-endo-dig cyclization strategy in a panel of primary screens. We observed a pure TLR8-agonistic activity profile in select furo[2,3-c] quinolines, with maximal potency conferred by a C2-butyl group (EC50 = 1.6 μM); shorter, longer, or substituted homologues as well as compounds bearing C1 substitutions were inactive, which was rationalized by docking studies using the recently described crystal structure of human TLR8. The best-in-class compound displayed prominent proinflammatory cytokine induction (including interleukin-12 and interleukin-18), but was bereft of interferon-α inducing properties, confirming its high selectivity for human TLR8.
SUBSTITUTED PYRIDINE DERIVATIVES, PHARMACEUTICAL COMPOSITIONS, AND METHODS OF USE TO TREAT OXIDATIVE STRESS
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Page/Page column 30, (2011/04/13)
Substituted pyridine derivatives, methods of their preparation, pharmaceutical compositions comprising a substituted pyridine derivative, and methods of use in treating inflammation are provided. The substituted pyridine derivatives may control of the act