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105902

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J Q Zhou et al.
Die Pharmazie, 61(10), 869-873 (2006-10-31)
Aim of this study was to investigate liver metabolism of with regard to para toluene-sulfonamide (PTS), CYP isoforms, P-glycoprotein (P-gp), and drug interactions. Known substrates, inducers and inhibitors of CYP and inhibitor of P-gp were employed and metabolites were determined
Doreen Richter et al.
Chemosphere, 71(8), 1574-1581 (2008-01-09)
Three sulfonamides -para-toluenesulfonamide (p-TSA), ortho-toluenesulfonamide (o-TSA) and benzenesulfonamide (BSA) - have recently been detected in groundwater within a catchment area of one drinking water treatment plant (DWTP), which is located downstream of a former sewage farm. The degradation pathways of
Isao Nishimori et al.
Bioorganic & medicinal chemistry letters, 17(13), 3585-3594 (2007-05-08)
DNA clones for the beta-class carbonic anhydrase (CA, EC 4.2.1.1) of Helicobactor pylori (hpbetaCA) were obtained. A recombinant hpbetaCA protein lacking the N-terminal 15-amino acid residues was produced and purified, representing a catalytically efficient CA. hpbetaCA was strongly inhibited (K(I)s
Mika Hilvo et al.
Journal of medicinal chemistry, 52(3), 646-654 (2009-02-06)
We have cloned and purified to homogeneity the latest member of the mammalian alpha-carbonic anhydrase (CA, EC 4.2.1.1) family, the mouse CA XV (mCA XV) protein. An investigation on the post-translational modifications of the enzyme has also been performed. The
İsmail Fidan et al.
Bioorganic & medicinal chemistry, 23(23), 7353-7358 (2015-11-05)
The inhibition of two human cytosolic carbonic anhydrase isozymes I and II, with some novel glycine and phenylalanine sulfonamide derivatives were investigated. Newly synthesized compounds G1-4 and P1-4 showed effective inhibition profiles with KI values in the range of 14.66-315μM
Isao Nishimori et al.
Bioorganic & medicinal chemistry letters, 16(8), 2182-2188 (2006-02-07)
A library of sulfonamides/sulfamates has been investigated for the inhibition of the carboxyterminal truncated form of the alpha-carbonic anhydrase (CA, EC 4.2.1.1) isolated from the gastric pathogen Helicobacter pylori (hpCA). This enzyme, incorporating 202 amino acid residues, showed a catalytic
A M van Haperen et al.
FEMS microbiology letters, 204(2), 299-304 (2001-12-04)
A bacterium capable of utilising p-toluenesulphonamide was isolated from activated sludge. The isolated strain designated PTSA was identified as a Pseudomonas sp. using chemotaxonomic and genetic studies. Pseudomonas PTSA grew on p-toluenesulphonamide in a chemostat with approximately 90% release of
G J Pinniger et al.
Journal of muscle research and cell motility, 26(2-3), 135-141 (2005-07-09)
We have examined the effects of N-benzyl-p-toluene sulphonamide (BTS), a potent and specific inhibitor of fast muscle myosin-II, using small bundles of intact fibres or single fibres from rat foot muscle. BTS decreased tetanic tension reversibly in a concentration-dependent manner
Hidehiko Fujisawa et al.
Chemistry (Weinheim an der Bergstrasse, Germany), 12(19), 5082-5093 (2006-04-22)
Lewis base catalyzed Mannich-type reaction between trimethylsilyl enol ethers and N-tosylaldimines is described. Nitrogen anions generated from amides or imides such as lithium benzamide or potassium phthalimide are found to be effective Lewis base catalysts in DMF at room temperature
Isao Nishimori et al.
Journal of medicinal chemistry, 49(6), 2117-2126 (2006-03-17)
We have cloned and sequenced Helicobacter pylori alpha-class carbonic anhydrase (hpCA) from patients with different gastric mucosal lesions, including gastritis (n=15), ulcer (n=6), and cancer (n=16). Although several polymorphisms were newly identified such as 12Ala, 13Thr, 16Ile, and 168Phe, there
Pascale Joseph et al.
Bioorganic & medicinal chemistry, 19(3), 1172-1178 (2011-01-22)
A β-carbonic anhydrase (CA, EC 4.2.1.1) from the bacterial pathogen Brucella suis, bsCA II, has been cloned, purified, and characterized kinetically. bsCA II showed high catalytic activity for the hydration of CO(2) to bicarbonate, with a k(cat) of 1.1×10(6), and
Alessio Innocenti et al.
Bioorganic & medicinal chemistry, 17(13), 4503-4509 (2009-05-20)
The beta-carbonic anhydrase (CA, EC 4.2.1.1) from the fungal pathogen Candida albicans (Nce103) is involved in a CO(2) sensing pathway critical for the pathogen life cycle and amenable to drug design studies. Herein we report an inhibition study of Nce103
B M Hausen et al.
Contact dermatitis, 33(3), 157-164 (1995-09-01)
Nail polish that has completely dried on the fingernails contains water-soluble components that attain the skin during extensive but transient contact. This was proven by water extraction of thin layers of nail polish that had been painted onto glass plates
G Luo et al.
Preparative biochemistry & biotechnology, 38(3), 265-270 (2008-06-24)
A series of 14-alkyl and aryl-14H-dibenzo[a.j]xanthenes have been synthesized with high yields through a one-pot condensation of beta-naphthol with alkyl or aryl aldehydes in the presence of BSA or o-TSA in a solvent-free medium.
Anthony Bertucci et al.
Bioorganic & medicinal chemistry, 17(14), 5054-5058 (2009-06-13)
The inhibition of a newly cloned coral carbonic anhydrase (CA, EC 4.2.1.1) has been investigated with a series of sulfonamides, including some clinically used derivatives (acetazolamide, methazolamide, ethoxzolamide, dichlorophenamide, dorzolamide, brinzolamide, benzolamide, and sulpiride, or indisulam, a compound in clinical
Jennifer A Jacobsen et al.
Journal of medicinal chemistry, 54(2), 591-602 (2010-12-30)
Fragment-based lead design (FBLD) has been used to identify new metal-binding groups for metalloenzyme inhibitors. When screened at 1 mM, a chelator fragment library (CFL-1.1) of 96 compounds produced hit rates ranging from 29% to 43% for five matrix metalloproteases
Jianxing He et al.
Anti-cancer drugs, 20(9), 838-844 (2009-08-12)
Para-toluenesulfonamide (PTS), active ingredient being PTS, is a new anticancer drug applied through local intratumoral injection. The aim of this phase II clinical trial was to investigate the response and toxicity of standard gemcitabine (GEM) plus cisplatin (CIS) chemotherapy with
Isao Nishimori et al.
Journal of medicinal chemistry, 52(9), 3116-3120 (2009-04-03)
The Rv3273 gene product of Mycobacterium tuberculosis, a beta-carbonic anhydrase (CA, EC 4.2.1.1), mtCA 3, shows appreciable catalytic activity for CO(2) hydration (k(cat) of 4.3 x 10(5) s(-1), and k(cat)/K(m) of 4.0 x 10(7) M(-1) x s(-1)). A series of
Isao Nishimori et al.
Bioorganic & medicinal chemistry, 15(23), 7229-7236 (2007-09-11)
The cytosolic human carbonic anhydrase (hCA, EC 4.2.1.1) isozyme III (hCA III) has been cloned and purified by the GST-fusion protein method. Recombinant pure hCA III had the following kinetic parameters for the CO(2) hydration reaction at 20 degrees C
Daniela Vullo et al.
Bioorganic & medicinal chemistry letters, 15(4), 971-976 (2005-02-03)
The inhibition of a newly cloned human carbonic anhydrase (CA, EC 4.2.1.1), isozyme VII (hCA VII), has been investigated with a series of aromatic and heterocyclic sulfonamides, including some of the clinically used derivatives (acetazolamide, methazolamide, ethoxzolamide, dichlorophenamide, dorzolamide, brinzolamide
Sarah L Rolland et al.
Dental materials : official publication of the Academy of Dental Materials, 23(12), 1468-1472 (2007-03-14)
This study aims to investigate the importance of ISO11405 recommended storage regime for extracted teeth in surface disinfectant chloramine T (chlT) prior to use in biofilm or in vitro caries studies involving microorganisms. ChlT may be absorbed into dentin and
Isao Nishimori et al.
Bioorganic & medicinal chemistry, 19(16), 5023-5030 (2011-07-16)
The two β-carbonic anhydrases (CAs, EC 4.2.1.1) from the bacterial pathogen Salmonella enterica serovar Typhimurium, stCA 1 and stCA 2, were investigated for their inhibition with a large panel of sulfonamides and sulfamates. Unlike inorganic anions, which are weak, millimolar
Olutosin R Idowu et al.
Journal of AOAC International, 87(5), 1098-1108 (2004-10-21)
Chloramine-T is a disinfectant being developed as a treatment for bacterial gill disease in cultured fish. As part of the drug approval process, a method is required for the confirmation of chloramine-T residues in edible fish tissue. The marker residue
A simple method of determining TS-F-R in nail polish.
B M Hausen
Contact dermatitis, 32(3), 188-190 (1995-03-01)
Zhan-Guo Chen et al.
The Journal of organic chemistry, 74(3), 1371-1373 (2008-12-26)
The regio- and stereoselective aminobromination of alpha,beta-unsaturated ketones catalyzed by copper powder has been established with 4-TsNH(2) and NBS as the nitrogen/bromine sources, respectively. This method provides an easy access for preparation of vicinal aminohalo derivatives in the presence of
G Li et al.
Acta chemica Scandinavica (Copenhagen, Denmark : 1989), 50(8), 649-651 (1996-08-01)
The p-toluenesulfonamide derivate of the C-13 side-chain of taxol was prepared on a one third mole scale in a single step from methyl cinnamate. The process employed is catalytic asymmetric aminohydroxylation (catalytic AA). In the present case, there is no
Jiang-Quan Zhou et al.
Acta pharmacologica Sinica, 27(5), 635-640 (2006-04-22)
To study the in vivo and in vitro metabolism and the effect of para-toluene-sulfonamide (PTS) on cytochrome P450 enzymes (CYP450). Total CYP450 and microsome protein content were determined after iv pretreatment of rats with PTS. CYP-specific substrates were incubated with
Yang Yang et al.
Organic letters, 13(20), 5608-5611 (2011-09-16)
BF(3)·OEt(2)-catalyzed direct cyanation of indoles and pyrroles using a less toxic, bench-stable, and easily handled electrophilic cyanating agent N-cyano-N-phenyl-para-toluenesulfonamide (NCTS) affords 3-cyanoindoles and 2-cyanopyrroles in good yields with excellent regioselectivity. The substrate scope is broad with respect to indoles and
Min-ying Li et al.
Nan fang yi ke da xue xue bao = Journal of Southern Medical University, 28(2), 249-251 (2008-02-06)
To investigate the dose-effect relationship of para-toluenesulfonamide (PTS) for treatment of hepatocellular carcinoma in rats. Forty-two SD rats bearing subcutaneous transplanted hepatocellular carcinoma were randomly divided into 6 groups (n=7), in which 0.02, 0.04, 0.06, 0.08, and 0.10 ml PTS
Anna Ohradanova et al.
Bioorganic & medicinal chemistry, 20(4), 1403-1410 (2012-01-31)
The α-carbonic anhydrase (CA, EC 4.2.1.1) Astrosclerin-3 previously isolated from the living fossil sponge Astrosclera willeyana (Jackson et al., Science 2007, 316, 1893), was cloned, kinetically characterized and investigated for its inhibition properties with sulfonamides and sulfamates. Astrosclerin-3 has a
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