Reactions of 5-phenyl-3(3H)-thioxo-1,2,4-dithiazole (1) with unsaturated and active phosphonium salts as well as with phosphonates, at r. t. and under the effect of basic catalysis, afforded mainly 1,3,5dithiazines 5, 12, 17a, 17b, 23a or 23b. Substituted 1,3-dithiol 7 and 1,3-thiazoles 13, 19a, 19b, 22a and 22b were isolated as by-products. 1,3,5-Dithiazine products showed pharmacological pote...

To find novel histone deacetylase 6 (HDAC6)-selective inhibitors and clarify the structural requirements for HDAC6-selective inhibition, we prepared thiolate analogues designed based on the structure of an HDAC6-selective substrate and evaluated the histone/alpha-tubulin acetylation selectivity by Western blot analysis. Aliphatic compounds 17b-20b selectively caused alpha-tubulin acetylation ov...

Solithromycin, a next-generation macrolide and novel fluoroketolide, was tested against a 2012 collection of serotyped U.S. macrolide-resistant Streptococcus pneumoniae isolates associated with community-acquired bacterial pneumonia (CABP). Against all 272 isolates, solithromycin demonstrated high potency (MIC50/90, 0.06/0.25 μg/ml), and it inhibited all strains at MICs of ≤0.5 μg/ml, including...

1 State Key Laboratory of Luminescence and Applications, Changchun Institute of Optics, Fine Mechanics and Physics, CAS.3888 East Nanhu Road, Changchun 130033, China 2 Beijing Key Laboratory for Green Catalysis and Separation, Department of Chemistry and Chemical Engineering, Beijing University of Technology, Beijing 100124, China 3 University of Chinese Academy of Sciences, No.19A Yuquan Road,...

Pirfenidone, a pyridone compound, is an effective and novel antifibrotic agent. In this article, we describe the design, synthesis and activity evaluation of novel antifibrotic agents, 1-(substituted aryl)-5-trifluoromethyl-2(1H) pyridones modified with carbohydrate. Most of the title compounds exhibited comparable or better inhibitory activity than fluorofenidone. Notably, compound 19a demonst...

Yafei Ning 1,2,*, Yunbin Yuan 1, Zhen Huang 3, Yanju Chai 1 and Bingfeng Tan 1,2 1 State Key Laboratory of Geodesy and Earth’s Dynamics, Institute of Geodesy and Geophysics, Chinese Academy of Sciences, Wuhan 430077, China; [email protected] (Y.Y.); [email protected] (Y.C.); [email protected] (B.T.) 2 University of Chinese Academy of Sciences, No. 19A Yuquan Road, Beijing 100049, China ...