53668-37-4Relevant academic research and scientific papers
Amino-(N-alkyl) benzsulfamide synthesis method
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Paragraph 0126-0129, (2017/04/14)
The invention discloses an amino-(N-alkyl) benzsulfamide synthesis method. The method comprises the steps of adding aminobenzenesul fonamide, an iridium complex catalyst, alkali, compound alcohol and the solvent tert-amyl alcohol into a reaction container for reaction lasting several hours at 120-150 DEG C, then reducing temperature to room temperature, conducting rotary evaporation to remove the solvent, and then conducting column separation to obtain the target compound. Commercial aminobenzenesul fonamide and nearly non-toxic compound alcohol are used as starting materials, only water is generated as reaction byproduct, and no environment harm is done; reaction atom economy is high.
Synthesis and biological evaluation of norcantharidin derivatives as protein phosphatase-1 inhibitors
Zhao, Jie,Guan, Xiao-Wen,Chen, Shi-Wu,Hui, Ling
, p. 363 - 366 (2015/02/19)
Cantharidin and norcantharidin display anticancer activity against a broad range of tumor cell lines. In this study, we have synthesized a series of norcantharidin derivatives and evaluated their cytotoxic effects on four human tumor cell lines together with the genetically normal human diploid fibroblast line WI-38. One of our compounds (1S,4R)-3-((4-(4-(4-fluorophenyl)piperazin-1-ylsulfonyl) phenyl)carbamoyl)-7-oxa-bicyclo[2.2.1]heptane-2-carboxylic acid (12) exhibited potent cytotoxic effects on the tumor cell lines A-549, HepG2, HeLa, and HCT-8, whereas it was less toxic to WI-38 cells than its parent compound, norcantharidin. In addition, this compound inhibited protein phosphatase-1 activity and microtubule formation in HeLa cells, and it also interacts with calf thymus DNA.
Effective Recognition of Different Types of Amino Groups: From Aminobenzenesulfonamides to Amino-(N-alkyl)benzenesulfonamides via Iridium-Catalyzed N-Alkylation with Alcohols
Lu, Lei,Ma, Juan,Qu, Panpan,Li, Feng
supporting information, p. 2350 - 2353 (2015/06/02)
(Chemical Equation Presented). A simple, highly efficient, and general strategy for the direct synthesis of amino-(N-alkyl)benzenesulfonamides has been accomplished via direct N-alkylation of aminobenzenesulfonamides bearing both different types of amino groups with alcohols as alkylating agents. Notably, this research exhibited the potential for the recognition of different types of amino groups in the N-alkylation of complex molecules with alcohols, facilitating the progress of the transition-metal-catalyzed "hydrogen autotransfer (or hydrogen-borrowing) process."
Synthesis and SAR of novel, 4-(phenylsulfamoyl)phenylacetamide mGlu 4 positive allosteric modulators (PAMs) identified by functional high-throughput screening (HTS)
Engers, Darren W.,Gentry, Patrick R.,Williams, Richard,Bolinger, Julie D.,Weaver, C. David,Menon, Usha N.,Conn, P. Jeffrey,Lindsley, Craig W.,Niswender, Colleen M.,Hopkins, Corey R.
scheme or table, p. 5175 - 5178 (2010/10/02)
Herein we disclose the synthesis and SAR of a series of 4-(phenylsulfamoyl)phenylacetamide compounds as mGlu4 positive allosteric modulators (PAMs) that were identified via a functional HTS. An iterative parallel approach to these compounds culminated in the discovery of VU0364439 (11) which represents the most potent (19.8 nM) mGlu4 PAM reported to date.
NOVEL ADENOSINE A3 RECEPTOR AGONISTS
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Page/Page column 33-34, (2008/06/13)
The invention realizes that a series of sulfonamido derivatives with a conserved uronamide group at the 5' position provide superior A3 receptor affinity as well as selectivity. These new adenosine agonists are sulfonamido deritatives N-substituted with aliphatic groups (cyclic or linear) or aromatic radicals.
Neuropeptide Y antagonists
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Page column 38, (2010/02/05)
The compound is a neuropeptide Y antagonist and is effective in treating feeding disorders, cardiovascular diseases and other physiological disorders.
