IntroductionTrazodone was authorized for the treatment of depression in the 1970s. Several additional therapeutic uses have been proposed due to its heterogeneous mechanism. This study aims to determine the use of trazodone in the elderly in Spain.
Trazodone is used as an antidepressant in doses between 150 and 600 mg. At lower doses, it is commonly used to treat insomnia. There are few case reports about confusional symptoms as an undesirable side effect of this drug. We report a case of a patient who presented with delirium after prescri...
In this work, the sulfonic acid (–SO3H) group terminated Fe3O4@SiO2 magnetic spheres were prepared. Polypyrrole (PPy) was in-situ polymerized on Fe3O4@SiO2–SO3H spheres due to the dual roles of the –SO3H groups: acting as both “anchoring sites” for adsorbing of pyrrole monomer and dopant ag...
The model tripeptide Boc-Gly-S-Ala-Aib-OMe (2b) and the two monothiated analogues Boc-Gly(1ψ2CSNH)-S-Ala-Aib-OMe (2c) and Boc-Gly-S-Ala(2ψ3 CSNH)-Aib-OMe (2a) were synthesized. Peptide 2a was obtained by thiation of 1a using 2,4-bis(4-methoxyphenyl)-1,3,2,4-dithiadiphosphetane 2,4-disulfide, L...
The synthesis of the decaendothiopeptide BOC-Trp-Ile-Ala-Aib-Ile-ValΨ[CSNH]Aib-Leu-Aib-Pro-OMe is described. The introduction of the thioamide group next to the bulky Aib occurred via a variation of the ‘azirine/oxazolone method’ without epimerisation. The structure of the decaendothiopeptide...
Two model peptides have been synthesized, a pentapeptide 1 (Boc-Gly-ΔZPhe-Leu-ΔZPhe-Ala-NHMe) and an octapeptide 2 (Boc-Val-ΔZPhe-Phe-Ala-ΔZPhe-Phe-Ala-Leu-Ala-gDZPhe-Leu-OMe). The conformations have been investigated in chloroform and dimethylsulfoxide by one and two dimensional NMR techniq...
The two model peptides Boc-S-Ala-Aib-S-Ala-OMe (1a) and Ac-S-Ala-Aib-S-Ala-OMe (1b) and their monothiated analogues Boc-S(R)-AlaΨ(CSNH)-Aib-S-Ala-OMe (3a), Boc-S-Ala-AibΨ(CSNH)-S-Ala-OMe (4a), AcΨ(CSNH)-S-Ala-Aib-S-Ala-OMe (2b), Ac-S-Ala-AibΨ(CSNH)-S-Ala-OMe (4b),and the dithiated Boc-S-AlaΨ...
Nandrolone and/or its precursors are included in the World Anti-doping Agency (WADA) list of forbidden substances and methods and as such their use is banned in sport. 19-Norandrosterone (19-NA) the main metabolite of these compounds can also be produced endogenously. The need to establish the o...
The dietary supplements 19-norandrostenedione and 19-norandrostenediol are potential metabolic precursors of nandrolone. They are considered by law in the United States as prohormones without proven therapeutic, curative or diagnostic properties, and therefore available as over-the-counter drugs...
Using n-PrPPh2 as the nucleophilic catalyst, the [4+2] cycloaddition reaction of the sulfamate-derived cyclic imines with allenoates works efficiently to yield various sulfamate-fused tetrahydropyridines in high yields with excellent diastereoselectivities. Using amino acid-based bifunctional ph...
Herein we report the synthesis of a new series of aromatic sulfamates investigated for the inhibition of four human (h) isoforms of zinc enzyme carbonic anhydrase (CA, EC 4.2.1.1), hCA I, II, IV, and IX. The reported derivatives, obtained by a sulfamoylation reaction of the corresponding phenoli...
Several model mechanism-based inhibitors (MbIs) were designed and evaluated for their ability to inhibit sulfatases. The MbI motifs were based on simple aromatic sulfates, which are known to be commonly accepted substrates across this highly conserved enzyme class, so that they might be generall...
A Brønsted acid-catalyzed asymmetric Friedel–Crafts alkylation of 3-indolylsulfamidates with indoles has been established toward the efficient synthesis of biologically important bisindolylarylmethane derivatives containing the phenylsulfamate group. The reaction using chiral BINOL-derived phos...
In the current work, we report the discovery of new sulfonate and sulfamate derivatives of benzofuran- and benzothiophene as potent inhibitors of human carbonic anhydrases (hCAs) II, IX and XII. A set of derivatives, 1a–t, having different substituents on the fused benzofuran and benzothiophene...
Four new series of aromatic sulfamates were synthesized and investigated for the inhibition of four human (h) isoforms of zinc enzyme carbonic anhydrase (CA, EC 4.2.1.1), hCA I, II, IX, and XII. The reported derivatives, obtained by a sulfamoylation reaction of the corresponding phenolic precurs...
Two new piperazinyl-ureido single ring aryl sulfamate-based inhibitor series were designed against the emerging oncology drug target steroid sulfatase (STS), for which there are existing potent steroidal and non-steroidal agents in clinical trials. 4-(Piperazinocarbonyl)aminosulfamates (5–31) w...
In the present article, we reviewed the sulfamate-containing compounds reported as bioactive molecules. The possible molecular targets of sulfamate derivatives include steroid sulfatase enzyme, carbonic anhydrases, acyl transferase, and others. Sulfamate derivatives can help treat hormone-depend...
Effective synthesis of novel sulfamates from various carboxylic acids has been developed in the presence of chlorosulfonyl isocyanate (CSI) in mild conditions. Several acids, bases and solvents effects were investigated for one-pot synthesis sulfamates as a catalyst. Finally, triflic acid was fo...
The interaction of bilirubin, biliverdin, bilirubin dimethyl ester, biliverdin dimethyl ester, xanthobilirubic acid, and xanthobilirubin methyl ester with trihydroxy and dihydroxy bile salt solutions is investigated by micellar electrokinetic chromatography (MEKC). The capacity factor of each co...
The characteristic thermodynamically-favored intramolecularly hydrogen-bonded conformation adopted by bilirubin pigments is destabilized by substituting methyl groups on the C(10) central methylene. These methyl groups impose conformation-destabilizing methyl-methylene non-bonded steric interact...
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