- Cu(II)-catalyzed decarboxylation/elimination of N-arylsulfonyl amino acids to primary aryl sulfonamides
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A novel protocol for CuO-catalyzed decarboxylation/elimination of N-arylsulfonyl amino acids was developed. It is the first example of using an accessible amino acid as an ammonia synthetic equivalent for the synthesis of primary aryl sulfonamides via oxidative decarboxylation/elimination reactions. The present protocol shows excellent functional group tolerance and provides an efficient method for the synthesis of primary aryl sulfonamides in excellent yields.
- Zhou, Liandi,Li, Xiaokang,Liu, Wei,Zhao, Yongli,Chen, Junmin
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p. 1299 - 1306
(2016/08/16)
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- Design and synthesis of benzenesulfonanilides active against methicillin-resistant Staphylococcus aureus and vancomycin-resistant Enterococcus
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Vancomycin is mainly used as an antibacterial agent of last resort, but recently vancomycin-resistant bacterial strains have been emerging. Although new antimicrobials have been developed in order to overcome drug-resistant bacteria, many are structurally
- Namba, Kensuke,Zheng, Xiaoxia,Motoshima, Kazunori,Kobayashi, Hidetomo,Tai, Akihiro,Takahashi, Eizo,Sasaki, Kenji,Okamoto, Keinosuke,Kakuta, Hiroki
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p. 6131 - 6144
(2008/12/21)
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- N-Acyl arylsulfonamides as novel, reversible inhibitors of human steroid sulfatase
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Steroid sulfatase (STS) is an attractive target for a range of oestrogen- and androgen-dependent diseases. In search of novel chemotypes of STS inhibitors, we had previously identified nortropinyl-arylsulfonylureas 1; however, while these compounds were good inhibitors of purified STS (lowest Ki = 76 nM), they showed only weak inhibition of STS activity in cells (lowest IC50 around 2 μM). Extended structure-activity relationship studies involving modification of the phenylacetyl side chain and replacement of the nortropine element by simpler scaffolds led to the discovery of N-acyl arylsulfonamides, more specifically N-(Boc-piperidine-4-carbonyl)- benzenesulfonamides, as STS inhibitors, some of which exhibit improved cellular potency (best IC50 = 270 nM).
- Lehr, Philipp,Billich, Andreas,Wolff, Barbara,Nussbaumer, Peter
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p. 1235 - 1238
(2007/10/03)
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- GLYT1 TRANSPORTER INHIBITORS AND USES THEREOF IN TREATMENT OF NEUROLOGICAL AND NEUROPSYCHIATRIC DISORDERS
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Use of a compound of formula (I): or a salt, solvate or a physiologically functional derivative thereof, for the manufacture of a medicament for treating a disorder mediated by GlyT1, such as foe example schizophrenia, is disclosed, wherein R1,
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Page/Page column 24; 25
(2008/06/13)
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