51230-92-3Relevant academic research and scientific papers
PhSO2SCF2H: A Shelf-Stable, Easily Scalable Reagent for Radical Difluoromethylthiolation
Zhu, Dianhu,Shao, Xinxin,Hong, Xin,Lu, Long,Shen, Qilong
supporting information, p. 15807 - 15811 (2016/12/16)
A new shelf-stable and easily scalable difluoromethylthiolating reagent S-(difluoromethyl) benzenesulfonothioate (PhSO2SCF2H) was developed. PhSO2SCF2H is a powerful reagent for radical difluoromethylthiolation of aryl and alkyl boronic acids, decarboxylative difluoromethylthiolation of aliphatic acids, and a phenylsulfonyl-difluoromethylthio difunctionalization of alkenes under mild reaction conditions.
Diaryl substituted pyrrolidinones and pyrrolones as 5-HT2C inhibitors: Synthesis and biological evaluation
Micheli, Fabrizio,Pasquarello, Alessandra,Tedesco, Giovanna,Hamprecht, Dieter,Bonanomi, Giorgio,Checchia, Anna,Jaxa-Chamiec, Albert,Damiani, Federica,Davalli, Silvia,Donati, Daniele,Gallotti, Chiara,Petrone, Marcella,Rinaldi, Marilisa,Riley, Graham,Terreni, Silvia,Wood, Martyn
, p. 3906 - 3912 (2008/12/21)
Within the continuous quest for the discovery of novel compounds able to treat anxiety and depression, the generation of a pharmacophore model for 5-HT2C receptor antagonists and the discovery of a new class of potent and selective 5-HT2C
Synthesis and structure-antifungal activity relationships of 3-aryl-5-alkyl-2,5-dihydrofuran-2-ones and their carbanalogues: Further refinement of tentative pharmacophore group
Pour, Milan,Spulak, Marcel,Balsanek, Vojtech,Kunes, Jiri,Kubanova, Petra,Buchta, Vladimir
, p. 2843 - 2866 (2007/10/03)
Two series of 3-(substituted phenyl)-5-alkyl-2,5-dihydrofuran-2-ones related to a natural product, (-)incrustoporine, were synthesized and their in vitro antifungal activity evaluated. The compounds with halogen substituents on the phenyl ring exhibited selective antifungal activity against the filamentous strains of Absidia corymbifera and Aspergillus fumigatus. On the other hand, the influence of the lenghth of the alkyl chain at C(5) was marginal. The antifungal effect of the most active compound against the above strains was higher than that of ketoconazole, and close to that of amphotericin B. In order to verify the hypothesis about a possible relationship between the Michael-accepting ability of the compounds and their antifungal activity, a series of simple carbanalogues, 2-(substituted phenyl)cyclopent-2-enones, was prepared and subjected to antifungal activity assay as well.
Antagonists of the human CCR5 receptor as anti-HIV-1 agents. Part 2: Structure-activity relationships for substituted 2-aryl-1-[N-(methyl)-N-(phenylsulfonyl)amino]-4-(piperidin-1-yl)butanes
Finke, Paul E.,Meurer, Laura C.,Oates, Bryan,Mills, Sander G.,MacCoss, Malcolm,Malkowitz, Lorraine,Springer, Martin S.,Daugherty, Bruce L.,Gould, Sandra L.,DeMartino, Julie A.,Siciliano, Salvatore J.,Carella, Anthony,Carver, Gwen,Holmes, Karen,Danzeisen, Renee,Hazuda, Daria,Kessler, Joseph,Lineberger, Janet,Miller, Michael,Schleif, William A.,Emini, Emilio A.
, p. 265 - 270 (2007/10/03)
(2S)-2-(3,4-Dichlorophenyl)-1-[N-(methyl)-N-(phenylsulfonyl)amino]-4-[spiro(2 ,3-dihydrobenzthiophene-3,4′-piperidin-1′yl)]butane S-oxide (3) has been identified as a potent CCR5 antagonist lead structure having an IC50 = 35 nM. Herein, we describe the structure-activity relationship studies directed toward the requirement for and optimization of the C-2 phenyl fragment. The phenyl was found to be important for CCR5 antagonism and substitution was limited to small moieties at the 3-position (13 and 16: X = H, 3-F, 3-Cl, 3-Me).
3-Phenyl-5-methyl-2H,5H-furan-2-ones: Tuning antifungal activity by varying substituents on the phenyl ring
Pour, Milan,Spulak, Marcel,Balsanek, Vojtech,Kunes, Jiri,Buchta, Vladimir,Waisser, Karel
, p. 1893 - 1895 (2007/10/03)
A series of racemic 3-phenyl-5-methyl-2H,5H-furan-2-ones related to a natural product, (-)incrustoporine, was synthesized, and their antifungal activity evaluated. The key structural feature, furanone ring, was closed via H2SO4-mediated cyclization of 2-phenylpent-4-enoic acids. The compounds displayed antifungal activity, especially against filamentous fungi. Expressed as the minimum inhibition concentration (MIC) in μmol/L, the activity of the most promising derivative against Absidia corymbifera matched that of ketoconazole (31.25 μmol/L). In terms of μg/mL, the substance was more active (7.6 μg/mL) than this standard antifungal drug (16.6 μg/mL). (C) 2000 Elsevier Science Ltd. All rights reserved.
