- Hydroxamic acid with benzenesulfonamide: An effective scaffold for the development of broad-spectrum metallo-β-lactamase inhibitors
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Given that β-lactam antibiotic resistance mediated by metallo-β-lactamases (MβLs) seriously threatens human health, we designed and synthesized nineteen hydroxamic acids with benzenesulfonamide, which exhibited broad-spectrum inhibition against four teste
- Li, Jia-Qi,Chen, Cheng,Yao, Min,Sun, Le-Yun,Gao, Han,Chigan, Jiazhu,Yang, Ke-Wu
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- Sequential C-S and S-N Coupling Approach to Sulfonamides
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A one-pot three-component reaction involving nitroarenes, (hetero)arylboronic acids, and potassium pyrosulfite leading to sulfonamides was described. A broad range of sulfonamides bearing different reactive functional groups were obtained in good to excellent yields through sequential C-S and S-N coupling that does not require metal catalysts.
- Chen, Kai,Chen, Wei,Han, Bing,Chen, Wanzhi,Liu, Miaochang,Wu, Huayue
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supporting information
p. 1841 - 1845
(2020/03/04)
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- Design, synthesis and biological activity of N-(3-substituted-phenyl)benzenesulfonamides as selective and reversible LSD1 inhibitors
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Lysine specific demethylase 1?plays a crucial role in regulating histone methylation at residues K4 and K9 on histone H3 and over-expresses in a variety of cancers. Here we designed, synthesized and evaluated a series of N-(3-substituted-phenyl)benzenesul
- Zha, Xiaoming,Wu, Liming,Xu, Siyuan,Zou, Fangxia,Xi, Jiayue,Ma, Tianfang,Liu, Rongfeng,Liu, Yu-Chih,Deng, Dawei,Gu, Yueqing,Zhou, Jinpei,Lan, Fei
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p. 2822 - 2831
(2016/11/09)
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- BENZIMIDAZOLECARBOXAMIDES AS INHIBITORS OF FAK
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This invention relates to benzimadolecarboxamides of formula (I) which are inhibitors of focal adhesion kinase, and as such are useful for treating proliferative diseases
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Page/Page column 26-27
(2010/11/17)
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- NOVEL COMPOUNDS, PHARMACEUTICAL COMPOSITIONS CONTAINING SAME, METHODS OF USE FOR SAME, AND METHODS FOR PREPARING SAME
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The present invention relates to a novel class of compounds comprising formula I, wherein n is 0 or 1. A is NR1, O, or S, wherein R1 is H, hydroxyl, C1-C10 alkyl, C1-C10 alkoxy, alkenyl, aryl, alkylaryl or arylalkyl. X is a carboxylate, a phosphonate, or a phosphate residue, or a C1-C10 alkyl residue optionally substituted with a carboxylate, phosphonate or phosphate residue. Y is a C1-C20 alkyl, alkenyl, halide, hydroxyl, C1-C20 alkoxy, aryl, alkylaryl, arylalkyl, cycloalkyl, cycloalkenyl, or a heterocyclic ring and is optionally substituted with one or more halides. Z is a H, a hydroxyl group, a halide, an aryl group, an alkylaryl group, an arylalkyl group, a cycloalkyl group, a cycloalkenyl group or a heterocyclic ring and is optionally substituted with one or more C1-C10 alkyl groups, C1-C10alkoxy groups, hydroxyl groups, cyano groups, carboxylate groups, halides, aryl groups, alkylaryl groups, arylalkyl groups, cycloalkyl groups, cycloalkenyl groups or heterocyclic rings.
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Page/Page column 34-35, 36
(2010/04/03)
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- Design and synthesis of small molecule glycerol 3-phosphate acyltransferase inhibitors
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The incidence of obesity and other diseases associated with an increased triacylglycerol mass is growing rapidly, particularly in the United States. Glycerol 3-phosphate acyltransferase (GPAT) catalyzes the ratelimiting step of glycerolipid biosynthesis, the acylation of glycerol 3-phosphate with saturated long-chain acyl-CoAs. In an effort to produce small molecule inhibitors of this enzyme, a series of benzoic and phosphonic acids was designed and synthesized. In vitro testing of this series has led to the identification of several compounds, in particular 2-(nonylsulfonamido)benzoic acid (15g), possessing moderate GPAT inhibitory activity in an intact mitochondrial assay.
- Wydysh, Edward A.,Medghalchi, Susan M.,Vadlamudi, Aravinda,Townsendd, Craig A.
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experimental part
p. 3317 - 3327
(2010/03/26)
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- NOVEL SULFONE AMIDE DERIVATIVES CAPABLE OF INHIBITING BACE
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The present invention relates to novel derivatives of sulfone amide of Formula 1 as defined in this disclosure which inhibit the activity of BACE (or beta-secretase). These sulfone amide derivatives are useful for the treatment and prevention of Alzheimer's disease and related diseases caused by production of beta-amyloid, by inhibiting the activity of BACE.
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Page/Page column 51-52
(2010/02/11)
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- Arylsulfonylaminobenzene derivatives and the use thereof as factor Xa inhibitors
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The present invention is directed to non-peptidic factor Xa inhibitors which are useful for the treatment of arterial and venous thrombotic occlusive disorders, inflammation, cancer, and neurodegenerative diseases. The factor Xa inhibitors provide compounds of structure: STR1 or pharmaceutically acceptable salts thereof; wherein R1 is alkyl, substituted alkyl, cycloalkyl, aryl, substituted aryl, heteroaryl or substituted heteroaryl; R2 is one of hydrogen, alkyl, cycloalkyl or aryl; R3 is one of hydrogen, hydroxy or alkoxy; R4 is one of --NH2, phenyl or pyridyl, wherein said phenyl and said pyridyl are optionally substituted with one or two of halogen, hydroxy, hydroxyalkyl, alkoxy, amino, monoalkylamino, dialkylamino, aminoalkyl, monoalkylaminoalkyl and/or dialkylaminoalkyl; X is one of --CH2 -- or --C(O)--; and n is from zero to eleven; provided that when R4 is --NH2, then R3 is hydrogen and n is other than zero; and also provided that when R3 is hydroxy or alkoxy, then R4 is other than --NH2, and n is other than zero.
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- Studies on Potential Antibacterial and Chelating Agents: Part III - Synthesis, Characterization and Biological Activity of Co(II), Ni(II) and Cu(II) Chelates with Some Sulphonamido and Benzamido Derivatives of Aminobenzoic Acids
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The complexing behaviour of some amidobenzoic acids towards Co(II), Ni(II) and Cu(II) has been studied.Eleven complexes of the type M(RH)2 where RH2 = o, m and p-benzenesulphonamidobenzoic acids, o-(p-toluenesulphonamido)benzoic acid and o-benzamidobenzoi
- Nandi, M. M.,Debnath, P.
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p. 498 - 501
(2007/10/02)
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