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Anthony Bertucci et al.
Bioorganic & medicinal chemistry letters, 21(2), 710-714 (2011-01-07)
The catalytic activity and the inhibition of a new coral carbonic anhydrase (CA, EC, from the scleractinian coral Stylophora pistillata, STPCA-2, has been investigated. STPCA-2 has high catalytic activity for the physiological reaction being less sensitive to anion and...
Ruth E Montes et al.
Electrophoresis, 29(16), 3325-3332 (2008-08-15)
This work expands the knowledge of the use of chemometric response surface methodology (RSM) in optimizing conditions for competitive binding partial filling ACE (PFACE). Specifically, RSM in the form of a Box-Behnken design was implemented in flow-through PFACE (FTPFACE) to...
Fabrizio Carta et al.
Bioorganic & medicinal chemistry letters, 19(23), 6649-6654 (2009-10-23)
The Rv3588c gene product of Mycobacterium tuberculosis, a beta-carbonic anhydrase (CA, EC denominated here mtCA 2, shows the highest catalytic activity for CO(2) hydration (k(cat) of 9.8 x 10(5)s(-1), and k(cat)/K(m) of 9.3 x 10(7)M(-1)s(-1)) among the three beta-CAs...
Padmakar V Khadikar et al.
Bioorganic & medicinal chemistry letters, 15(4), 931-936 (2005-02-03)
A novel use of NMR chemical shift of the SO(2)NH(2) protons (in dioxane as solvent) as a molecular descriptor is described for modeling the inhibition constant for benzene sulfonamides against the zinc enzyme carbonic anhydrase (CA, EC The methodology...
Raffaella Meffe et al.
Water research, 44(1), 205-213 (2009-09-22)
A finite element model was set-up to determine degradation rate constants for p-TSA during rapid sand filtration (RSF). Data used for the model originated from a column experiment carried out in the filter hall of a drinking water treatment plant...
An efficient FeCl3 -catalyzed amidation reaction of secondary benzylic and allylic alcohols with carboxamides or p-toluenesulfonamide.
Jana U, et al.
Tetrahedron Letters, 42(37), 6433-6435 (2001)
Dingben Chen et al.
The Journal of organic chemistry, 75(16), 5768-5771 (2010-07-30)
A copper-catalyzed cascade method has been developed to synthesize the 2H-benzo[b][1,4]thiazin-3(4H)-ones from 2-halo-N-(2-halophenyl)-acetamides 1 and AcSH via the S(N)2/deacetylation/coupling process, and to synthesize the quinoxalin-2(1H)-ones from 1 and TsNH(2) via the S(N)2/coupling/desulfonation process. The target products were obtained with diversity...
Isao Nishimori et al.
Journal of medicinal chemistry, 50(2), 381-388 (2007-01-19)
The secretory isozyme of human carbonic anhydrase (hCA, EC, hCA VI, has been cloned, expressed, and purified in a bacterial expression system. The kinetic parameters for the CO2 hydration reaction proved hCA VI to possess a kcat of 3.4...
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...
Arthur J Catino et al.
Organic letters, 7(13), 2787-2790 (2005-06-17)
[reaction: see text] A mild, efficient, and selective aziridination of olefins catalyzed by dirhodium(II) caprolactamate [Rh(2)(cap)(4).2CH(3)CN] is described. Use of p-toluenesulfonamide (TsNH(2)), N-bromosuccinimide (NBS), and potassium carbonate readily affords aziridines in isolated yields of up to 95% under extremely mild...
Charles H Reynolds et al.
Journal of medicinal chemistry, 51(8), 2432-2438 (2008-04-03)
Ligand efficiency (i.e., potency/size) has emerged as an important metric in drug discovery. In general, smaller, more efficient ligands are believed to have improved prospects for good drug properties (e.g., bioavailability). Our analysis of thousands of ligands across a variety...
Allergenic ingredients in nail polishes.
S B Levy
Contact dermatitis, 38(5), 303-303 (1998-07-17)
Pascale Joseph et al.
Journal of medicinal chemistry, 53(5), 2277-2285 (2010-02-18)
A beta-carbonic anhydrase (CA, EC from the bacterial pathogen Brucella suis, bsCA 1, has been cloned, purified, and characterized kinetically. bsCA 1 has appreciable activity as catalyst for the hydration of CO(2) to bicarbonate, with a k(cat) of 6.4...
Tomoko Minakuchi et al.
Journal of medicinal chemistry, 52(8), 2226-2232 (2009-03-26)
The beta-carbonic anhydrase (CA, EC encoded by the gene Rv1284 (mtCA 1) of Mycobacterium tuberculosis shows appreciable catalytic activity for CO(2) hydration, with a k(cat) of 3.9 x 10(5) s(-1) and a k(cat)/K(m) of 3.7 x 10(7) M(-1) s(-1)....
J R Meinertz et al.
Journal of AOAC International, 84(5), 1332-1336 (2001-10-17)
Chloramine-T is an effective drug for controlling fish mortality caused by bacterial gill disease. As part of the data required for approval of chloramine-T use in aquaculture, depletion of the chloramine-T marker residue (para-toluenesulfonamide; p-TSA) from edible fillet tissue of...
Yohei Munei et al.
Bioorganic & medicinal chemistry letters, 21(1), 141-144 (2010-12-07)
We proposed a novel QSAR (quantitative structure-activity relationship) procedure called LERE (linear expression by representative energy terms)-QSAR involving molecular calculations such as ab initio fragment molecular orbital and generalized Born/surface area ones. We applied LERE-QSAR to two datasets for the...
Daniela Vullo et al.
Bioorganic & medicinal chemistry letters, 15(4), 963-969 (2005-02-03)
The inhibition of a newly cloned human carbonic anhydrase (CA, EC, isozyme XII (hCA XII), has been investigated with a series of sulfonamides, including some clinically used derivatives (acetazolamide, methazolamide, ethoxzolamide, dichlorophenamide, dorzolamide, brinzolamide, benzolamide, and sulpiride, or indisulam...
Padmakar V Khadikar et al.
Bioorganic & medicinal chemistry letters, 15(4), 923-930 (2005-02-03)
The binding constants (logK) of benzene sulfonamides to human CA-II have been modeled using a large series of distance-based topological indices. The need or otherwise of the hydrophobic parameter (logP) for such topological modeling of logK has been examined critically....
Isao Nishimori et al.
Journal of medicinal chemistry, 48(24), 7860-7866 (2005-11-24)
A lately discovered carbonic anhydrase (hCA, EC, the mitochondrial hCA VB, was cloned, expressed, and purified. Kinetic parameters proved it to be 3.37 times more effective than hCA VA as a catalyst for the physiological reaction, with kcat =...
Vjacheslav M Petrov et al.
The journal of physical chemistry. A, 112(13), 2969-2976 (2008-02-28)
The molecular structure and conformational properties of para-methylbenzene sulfonamide (4-MBSA) and ortho-methylbenzene sulfonamide (2-MBSA) have been studied by gas electron diffraction (GED) and quantum chemical methods (B3LYP/6-311+G** and MP2/6-31G**). Quantum chemical calculations predict the existence of two conformers for 4-MBSA...
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...
Semra Isik et al.
Bioorganic & medicinal chemistry, 17(3), 1158-1163 (2009-01-07)
The protein encoded by the Nce103 gene of Saccharomyces cerevisiae, a beta-carbonic anhydrase (CA, EC designated as scCA, has been cloned, purified, characterized kinetically and investigated for its inhibition with a series of sulfonamides and one sulfamate. The enzyme...
J R Meinertz et al.
Journal of AOAC International, 82(5), 1064-1070 (1999-10-08)
Chloramine-T (N-sodium-N-chloro-p-toluene-sulfonamide) is a candidate therapeutic drug for treating bacterial gill disease, a predominant disease of a variety of fish species. Research has been initiated to obtain the U.S. Food and Drug Administration's (FDA) approval for the use of chloramine-T...
Anna Ohradanova et al.
Bioorganic & medicinal chemistry, 20(4), 1403-1410 (2012-01-31)
The α-carbonic anhydrase (CA, EC 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...
Hui Meng et al.
Nan fang yi ke da xue xue bao = Journal of Southern Medical University, 29(5), 1024-1025 (2009-05-23)
To study the effect of of percutaneous para-toluenesulfonamide (PTS) injection on transplanted hepatocarcinoma in nude mice. Sixty nude mice with subcutaneous transplanted hepatocarcinoma were randomized into 6 groups, namely PTS, chemotherapy, radiotherapy, PTS+chemotherapy, PTS+radiotherapy and control groups. PTS were injected...
Christian Lorber et al.
Inorganic chemistry, 46(8), 3192-3202 (2007-03-17)
p-Toluenesulfonamide (p-TsNH2) was successfully employed as an imido ligand precursor in the synthesis of highly air- and moisture-sensitive titanium(IV) and vanadium(IV) complexes. Reaction of M(NMe2)4 (M = Ti, V) with TsNH2 in toluene afforded [M(micro-NTs)(NMe2)2]2 dimer complexes (M = Ti...
Isao Nishimori et al.
Bioorganic & medicinal chemistry, 15(23), 7229-7236 (2007-09-11)
The cytosolic human carbonic anhydrase (hCA, EC 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...
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...
E Simone et al.
Lab on a chip, 18(15), 2235-2245 (2018-06-28)
In this work, a novel multi-microfluidic crystallization platform called MMicroCryGen is presented, offering a facile methodology for generating individual crystals for fast and easy screening of the polymorphism and crystal habit of solid compounds. The MMicroCryGen device is capable of...
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 family, the mouse CA XV (mCA XV) protein. An investigation on the post-translational modifications of the enzyme has also been performed. The...
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