32868-31-8Relevant articles and documents
Synthesis and Characterization of Azidobenzphetamine Analogs of the Cytochrome P450 Substrate Benzphetamine
Hodek, Petr,Strobel, Henry W.
, p. 253 - 267 (1994)
Benzphetamine, an amphetamine with sympathomimetic stimulant activity in the central nervous system, is a substrate for cytochromes P450 with highest metabolic turnover being catalyzed by cytochrome P4502B1.We synthesized three photolabile azido-compound
Synthesis of small molecule CDC25 phosphatases inhibitors
Contour-Galcéra, Marie-Odile,Lavergne, Olivier,Brezak, Marie-Christine,Ducommun, Bernard,Prévost, Grégoire
, p. 5809 - 5812 (2004)
A targeted library of 2-(4-nitrophenyl)ethylbenzylamines has been prepared to optimize the biological activity of BN82002, our initial lead compound, recently described as an original inhibitor of CDC25 phosphatases. The most potent of these compounds inhibit CDC25 in the micromolar range. A targeted library of small molecules has been prepared to optimize the biological activity of BN82002, our initial lead compound, recently described as an original inhibitor of CDC25 phosphatases. Some of these compounds inhibit CDC25 in the micromolar range and therefore reinforce the interest of CDC25 as an anticancer target.
SMALL MOLECULE DUAL-INHIBITORS OF TRPV4 AND TRPA1 FOR SANITIZING AND ANESTHETIZING
-
Paragraph 00230; 00234, (2017/11/04)
Provided are methods of sanitizing a subject, and methods of anesthetizing a subject. Further provided are methods of treating and/or preventing dermatological disorders, reducing skin inflammation, reducing pain, and/or reducing itch in a subject in need
TRPA1 AND TRPV4 INHIBITORS AND METHODS OF USING THE SAME FOR ORGAN-SPECIFIC INFLAMMATION AND ITCH
-
Paragraph 00162, (2016/03/18)
Provided are methods of treating and/or preventing dermatological disorders. Provided are methods of reducing skin inflammation, reducing pain, and/or reducing itch in a subject in need thereof. The methods may include administering to the subject an effe
TRPA1 AND TRPV4 INHIBITORS AND METHODS OF USING THE SAME FOR ORGAN-SPECIFIC INFLAMMATION AND ITCH
-
Paragraph 0192; 0193; 0194; 0201; 0202, (2016/12/12)
Provided are methods of treating and/or preventing dermatological disorders. Provided are methods of reducing skin inflammation, reducing pain, and/or reducing itch in a subject in need thereof. The methods may include administering to the subject an effe
Anti-Markovnikov hydroamination and hydrothiolation of electron-deficient vinylarenes catalyzed by well-defined monomeric copper(I) amido and thiolate complexes
Munro-Leighton, Colleen,Delp, Samuel A.,Alsop, Nikki M.,Blue, Elizabeth D.,Gunnoe, T. Brent
, p. 111 - 113 (2008/09/19)
Monomeric Cu(I) amido and thiolate complexes that are supported by the N-heterocyclic carbene ligand 1,3-bis(2,6-diisopropylphenyl)imidazol-2-ylidene (IPr) catalyze the hydroamination and hydrothiolation of electron-deficient vinylarenes with reactivity patterns that are consistent with an intermolecular nucleophilic addition of the amido/thiolate ligand of (IPr)Cu(XR) (X = NH or S; R = Ph, CH2Ph) to free vinylarene. The Royal Society of Chemistry.
New p-methylsulfonamido phenylethylamine analogues as class III antiarrhythmic agents: Design, synthesis, biological assay, and 3D-QSAR analysis
Liu, Hong,Ji, Ming,Luo, Xiaomin,Shen, Jianhua,Huang, Xiaoqin,Hua, Weiyi,Jiang, Hualiang,Chen, Kaixian
, p. 2953 - 2969 (2007/10/03)
Class III antiarrhythmic agents selectively delay the effective refractory period (ERP) and increase the transmembrance action potential duration (APD). Using dofetilide (2) as a template of class III antiarrhythmic agents, we designed and synthesized 16 methylsulfonamido phenylethylamine analogues (4a-d and 5a-1). Pharmacological assay indicated that all of these compounds showed activity for increasing the ERP in isolated animal atrium; among them, the effective concentration of compound 4a is 1.6 × 10-8 mol/L in increasing ERP by 10 ms, slightly less potent than that of 2, 1.1 × 10-8 mol/L. Compound 4a also produced a slightly lower change in ERP at 10-5 M, ΔERP% = 17.5% (ΔERP% = 24.0% for dofetilide). On the basis of this bioassay result, these 16 compounds together with dofetilide were investigated by the three-dimensional quantitative structure-activity relationship (3D-QSAR) techniques of comparative molecular field analysis (CoMFA), comparative molecular similarity index analysis (CoMSIA), and the hologram QSAR (HQSAR). The 3D-QSAR models were tested with another 11 compounds (4e-h and 5m-s) that we synthesized later. Results revealed that the CoMFA, CoMSIA, and HQSAR predicted activities for the 11 newly synthesized compounds that have a good correlation with their experimental value, r2 = 0.943, 0.891, and 0.809 for the three QSAR models, respectively. This indicates that the 3D-QSAR models proved a good predictive ability and could describe the steric, electrostatic, and hydrophobic requirements for recognition forces of the receptor site. On the basis of these results, we designed and synthesized another eight new analogues of methanesulfonamido phenylethyamine (6a-h) according to the clues provided by the 3D-QSAR analyses. Pharmacological assay indicated that the effective concentrations of delaying the ERP by 10 ms of these newly designed compounds correlated well with the 3D-QSAR predicted values. It is remarkable that the percent change of delaying ERP at 10-5 M compound 6c is much higher than that of dofetilide; the effective concentration of compound 6c is 5.0 × 10-8mol/L in increasing the ERP by 10 ms, which is slightly lower than that of 2. The results showed that the 3D-QSAR models are reliable and can be extended to design new antiarrhythmic agents.
ISOTHIOUREA DERIVATIVES USEFUL IN THERAPY
-
, (2008/06/13)
There are provided novel compounds of formula I, wherein D, R1, R2, R3, X and p are as defined in the specification together with processes for their preparation, compositions containing them and their use in therapy. Compounds of formula I are expected t
Substituent effects on the benzyl groups in Sommelet-Hauser rearrangement
Tanaka,Shirai,Sato
, p. 518 - 520 (2007/10/02)
The effects of substituents (MeO, Me, H, Br, CN, NO2) of the benzyl groups in the Sommelet-Hauser rearrangement of N,N-bis(substituted benzyl)-N-methyl(trimethylsilyl)methylammonium halides with cesium fluoride in N,N-dimethylformamide were exa
