13626-17-0Relevant articles and documents
Discovery of 2,4-dimethoxypyridines as novel autophagy inhibitors
Robke, Lucas,Rodrigues, Tiago,Schr?der, Peter,Foley, Daniel J.,Bernardes, Gon?alo J.L.,Laraia, Luca,Waldmann, Herbert
, p. 4531 - 4537 (2018)
Autophagy is a catabolic process, which mediates degradation of cellular components and has important roles in health and disease. Therefore, small molecule modulators of autophagy are in great demand. Herein, we describe a phenotypic high-content screen for autophagy inhibitors, which led to the discovery of a dimethoxypyridine-based class of autophagy inhibitors, which derive from previously reported, natural product-inspired MAP4K4 inhibitors. Comprehensive structure-activity relationship studies led to a potent compound, and biological validation experiments indicated that the mode of action was upstream or independent of mTOR.
BIARYL DERIVATIVE AND MEDICINE CONTAINING SAME
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Paragraph 0676; 0678, (2018/08/07)
Provided is a compound showing excellent antifungal activity against Trichophyton fungus, which is a major causative microorganism of superficial mycosis, and high effectiveness on diseases caused by Trichophyton fungi. A biaryl derivative represented by the formula (I) or a salt thereof: wherein ring A is an optionally substituted phenyl, or an optionally substituted 5- or 6-membered ring heteroaryl (ring A may be further condensed to form an optionally substituted fused ring); Q is CH2, C=O, NH, O, S or the like; X1, X2 and X3 are CR1 or N; Y is CH or N; Z is CR2b or N; R2a and R2b are each a hydrogen atom, a halogen atom, an optionally substituted C1-C6 alkyl group, a C1-C6 haloalkyl group or the like; R2a and R2b may form, together with carbon atoms bonded thereto, an optionally substituted carbocycle, or an optionally substituted heterocycle.
4-(N,N-dimethylamino)pyridine-embedded nanoporous conjugated polymer as a highly active heterogeneous organocatalyst
Zhang, Yuan,Zhang, Yong,Sun, Ya Lei,Du, Xin,Shi, Jiao Yi,Wang, Wei,Wang, Wei David
supporting information; experimental part, p. 6328 - 6334 (2012/06/18)
We report herein for the first time the incorporation of a versatile organocatalyst, 4-(N,N-dimethylamino)pyridine (DMAP), into the network of a nanoporous conjugated polymer (NCP) by the "bottom-up" approach. The resulting DMAP-NCP material possesses highly concentrated and homogeneously distributed DMAP catalytic sites (2.02 mmol g-1). DMAP-NCP also exhibits enhanced stability and permanent porosity due to the strong covalent linkage and the rigidity of the "bottom-up" monomers. As a result, DMAP-NCP shows excellent catalytic activity in the acylation of alcohols with yields of 92-99 %. The DMAP-NCP catalyst could be easily recovered from the reaction mixture and reused in at least 14 consecutive cycles without measurable loss of activity. Moreover, the catalytic acylation reaction could be performed under neat and continuous-flow conditions for at least 536 h of continuous work with the same catalyst activity. Copyright