- 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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- Deoxygenative Arylation of Carboxylic Acids by Aryl Migration
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An unprecedented deoxygenative arylation of aromatic carboxylic acids has been achieved, allowing the construction of an enhanced library of unsymmetrical diaryl ketones. The synergistic photoredox catalysis and phosphoranyl radical chemistry allows for precise cleavage of a stronger C?O bond and formation of a weaker C?C bond by 1,5-aryl migration under mild reaction conditions. This new protocol is independent of substrate redox-potential, electronic, and substituent effects. It affords a general and promising access to 60 examples of synthetically versatile o-amino and o-hydroxy diaryl ketones under redox-neutral conditions. Furthermore, it also brings one concise route to the total synthesis of quinolone alkaloid, (±)-yaequinolone A2, and a viridicatin derivative in satisfying yields.
- Ruzi, Rehanguli,Ma, Junyang,Yuan, Xiang-Ai,Wang, Wenliang,Wang, Shanshan,Zhang, Muliang,Dai, Jie,Xie, Jin,Zhu, Chengjian
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supporting information
p. 12724 - 12729
(2019/11/05)
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- SMALL MOLECULE INHIBITORS OF MCL-1 AND USES THEREOF
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This invention is in the field of medicinal chemistry. In particular, the invention relates to a new class of small-molecules having benzoic acid structure which function as inhibitors of Mcl-1 protein, and their use as therapeutics for the treatment of cancer and other diseases.
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Page/Page column 70-71; 76
(2016/11/14)
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- Synthesis and structure-activity relationships of o-sulfonamido- arylhydrazides as inhibitors of LL-diaminopimelate aminotransferase (LL-DAP-AT)
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Recently, ll-diaminopimelate aminotransferase (ll-DAP-AT), a pyridoxal-5′-phosphate (PLP)-dependent enzyme, was reported to catalyze a key step in the biosynthesis of l-lysine in plants and Chlamydia. Previous screening of a 29201-compound library against
- Fan, Chenguang,Vederas, John C.
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supporting information; experimental part
p. 5815 - 5819
(2012/08/28)
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- Inhibition effect of imidazoline and hydropyrimidine derivatives on the corrosion of brass in 0.6 M aqueous sodium chloride solution
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The inhibition effect of o-aminobenzoic acid (1), p-aminobenzoic acid (2), o-benzenesulphonamidobenzoic acid (3), p-benzenesulphonamidobenzoic acid (4), 2-(o-benzenesulphonamido)phenylimidazoline (5), 2-(p-benzenesulphonamido) phenylimidazoline (6), 2-(o-
- Ranjana,Banerjee, Ranu,Nandi
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p. 229 - 238
(2012/11/07)
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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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- Discovery of new chemical leads for selective EP1 receptor antagonists
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A series of 4-({2-[alkyl(phenylsulfonyl)amino]phenoxy}methyl)benzoic acids were identified as functional PGE2 antagonists with selectivity for the EP1 receptor subtype starting from a chemical lead 1, which was found while screening our in-house compound library. Discovery of the optimized analogs 21-23 is presented here and structure-activity relationships (SAR) are also discussed.
- Naganawa, Atsushi,Saito, Tetsuji,Nagao, Yuuki,Egashira, Hiromu,Iwahashi, Maki,Kambe, Tohru,Koketsu, Masatoshi,Yamamoto, Hiroshi,Kobayashi, Michiyoshi,Maruyama, Takayuki,Ohuchida, Shuichi,Nakai, Hisao,Kondo, Kigen,Toda, Masaaki
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p. 5562 - 5577
(2007/10/03)
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- Direct conversion of azides to carbamates and sulfonamides using Fe/NH4Cl: Effect of sonication
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A simple, direct and effective conversion of azides to carbamates and sulfonamides is achieved using Fe/NH4Cl in methanol. The influence of sonication and direct application in solution phase combinatorial chemistry are also studied by developing a 6x4 matrix library. (C) 2000 Elsevier Science Ltd.
- Chandrasekhar,Narsihmulu
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p. 7969 - 7972
(2007/10/03)
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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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