- Preparation method of sulfaquinoxaline
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The invention discloses a preparation method of sulfaquinoxaline. The preparation method comprises the following steps: mixing o-phenylenediamine, chloroacetic acid, an alkaline ionic liquid and a solid base catalyst; under the condition of continuously blowing in air, carrying out reaction for 1-5 hours at 80-150 DEG C; after the reaction, stopping blowing in air, and adding phosphorus oxychloride and p-amino-benzene sulfonamide to carry out reaction continuously for 1-3 hours at 80-150 DEG C; and carrying out separation and purification on a reaction liquid to obtain sulfaquinoxaline. The preparation method disclosed by the invention is easy to operate, has low requirements on reaction equipment and causes little pollution to the environment, the product is easy to separate, and the ionic liquid and solid base can be used repeatedly, so that the preparation method is an economical, practical, and environment-friendly technology.
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Paragraph 0027; 0028
(2016/11/21)
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- Discovering novel chemical inhibitors of human cyclophilin A: Virtual screening, synthesis, and bioassay
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Cyclophilin A (CypA) is a member of cyclophilins, a family of the highly homologous peptidyl prolyl cis-trans isomerases (PPIases), which can bind to cyclosporin A (CsA). CypA plays critical roles in various biological processes, including protein folding, assembly, transportation, regulation of neuron growth, and HIV replication. The discovery of CypA inhibitor is now of a great special interest in the treatment of immunological disorders. In this study, a series of novel small molecular CypA inhibitors have been discovered by using structure-based virtual screening in conjunction with chemical synthesis and bioassay. The SPECS_1 database containing 85,000 small molecular compounds was searched by virtual screening against the crystal structure of human CypA. After SPR-based binding affinity assay, 15 compounds were found to show binding affinities to CypA at submicro-molar or micro-molar level (compounds 1-15). Seven compounds were selected as the starting point for the further structure modification in considering binding activity, synthesis difficulty, and structure similarity. We thus synthesized 40 new small molecular compounds (1-6, 15, 16a-q, 17a-d, and 18a-l), and four of which (compounds 16b, 16h, 16k, and 18g) showed high CypA PPIase inhibition activities with IC50s of 2.5-6.2 μM. Pharmacological assay indicated that these four compounds demonstrated somewhat inhibition activities against the proliferation of spleen cells.
- Li, Jian,Chen, Jing,Gui, Chunshan,Zhang, Li,Qin, Yu,Xu, Qiang,Zhang, Jian,Liu, Hong,Shen, Xu,Jiang, Hualiang
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p. 2209 - 2224
(2007/10/03)
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- Process for formulating a synthetic drug for use in animal feed, and resulting formulation
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A method of formulating a synthetic drug for use in animal feed, for the purpose of reducing carry-over of the synthetic drug to subsequent lots of animal feed in the feed mill.
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