- Pyridine azo disperse dye containing sulfonic acid ester or sulfamine as well as synthesis method of pyridine azo disperse dye
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The invention provides pyridine azo disperse dye containing sulfonic acid ester or sulfamine as well as a preparation method of pyridine azo disperse dye. The molecular structure of the compound is asshown in the following formula: (the formula is as shown in the description). The synthesis method comprises the following steps: taking 3-nitrobenzene sulfonyl chloride or 3-nitryl-4-substituted benzene sulfony chloride, alcohol, phenol or primary amine, 3-cyan-4-methyl-6-hydroxyl-2-pyrifone or 3-cyan-4-methyl-hydroxyl-N-alkyl-2-pyridone as raw materials, performing sulfonic acid esterificationor sulfonic amidation, performing nitro reduction and performing diazotization coupling to obtain a product. The product provided by the invention is novel in structure, simple in synthesis, low in cost and suitable for industrialized production.
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Paragraph 0017
(2018/05/16)
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- Synthesis and Antitubulin Activity of N1- and N 4-Substituted 3,5-Dinitro Sulfanilamides against African Trypanosomes and Leishmania
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Thirty analogues of N1-phenyl-3,5-dinitro-N4,N 4-di-n-propylsulfanilamide (GB-II-5, compound 3), a new antikinetoplastid antimitotic agent, have been synthesized and evaluated. The addition of simple functional groups to the N1 aromatic ring generally decreases antiparasitic and antimitotic potency, but placement of a dibutyl substituent at the N4 nitrogen to give N1-phenyl-3,5-dinitro-N 4,N4-di-n-butylsulfanilamide (compound 35) augments antitrypanosomal and antileishmanial activity. Compound 35 possesses IC 50 values of 0.12 and 2.6 μM against cultured T. brucei and L. donovani amastigote-like forms, surpassing the activity of compound 3 against these parasites by 3.4- and 1.9-fold, respectively. Compound 35 inhibits the assembly of leishmanial tubulin with an IC50 of 6.9 μM and displays antimitotic effects in cultured T. brucei as assessed by flow cytometry, but shows little effect on purified mammalian tubulin, and displays 100-fold selectivity for trypanosomes over two mammalian cell lines. Although 3 and 35 were not effective in initial in vivo antitrypanosomal assays, the in vitro potency and selectivity of these compounds make N 1-aryl-3,5-dinitro-N4,N4-dialkylsulfanilamides a promising new class of antikinetoplastid agents that act on parasite tubulin.
- Bhattacharya, Gautam,Herman, Johnathan,Delfín, Dawn,Salem, Manar M.,Barszcz, Todd,Mollet, Mike,Riccio, Guy,Brun, Reto,Werbovetz, Karl A.
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p. 1823 - 1832
(2007/10/03)
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- New compounds
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The present invention relates to substituted bis-arylsulfonamide and arylsulfonamide compounds of the general formula (I) or the formula (II), which compounds are potentially useful for the prophylaxis and treatment of medical conditions relating to obesity, type II diabetes and/or disorders of the central nervous system.
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- Bicyclic heterocycles, the preparation thereof, and their use as pharmaceuticals
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The present invention relates to 5-membered heterocyclic condensed benzoderivatives of formula wherein Ra to Rc, A, X and Y are defined as in claim 1, the tautomers, stereoisomers, mixtures thereof and the salts thereof, particularly the physiologically acceptable salts thereof with inorganic or organic acids or bases which have valuable properties. The compounds of the above formula I wherein Rc denotes a cyano group are valuable intermediates for preparing the other compounds of formula I, and the compounds of the above formula I wherein Rc denotes one of the following amidino groups and the tautomers and stereoisomers thereof have valuable pharmacological properties, particularly an antithrombotic activity.
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