- 4-Sulfamoylphenylalkylamides as Inhibitors of Carbonic Anhydrases Expressed in Vibrio cholerae
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A current issue of antimicrobial therapy is the resistance to treatment with worldwide consequences. Thus, the identification of innovative targets is an intriguing challenge in the drug and development process aimed at newer antimicrobial agents. The state-of-art of anticholera therapy might comprise the reduction of the expression of cholera toxin, which could be reached through the inhibition of carbonic anhydrases expressed in Vibrio cholerae (VchCAα, VchCAβ, and VchCAγ). Therefore, we focused our interest on the exploitation of sulfonamides as VchCA inhibitors. We planned to design and synthesize new benzenesulfonamides based on our knowledge of the VchCA catalytic site. The synthesized compounds were tested thus collecting useful SAR information. From our investigation, we identified new potent VchCA inhibitors, some of them displayed high affinity toward VchCAγ class, for which few inhibitors are currently reported in literature. The best interesting VchCAγ inhibitor (S)-N-(1-oxo-1-((4-sulfamoylbenzyl)amino)propan-2-yl)furan-2-carboxamide (40) resulted more active and selective inhibitor when compared with acetazolamide (AAZ) as well as previously reported VchCA inhibitors.
- Mancuso, Francesca,De Luca, Laura,Bucolo, Federica,Vrabel, Milan,Angeli, Andrea,Capasso, Clemente,Supuran, Claudiu T.,Gitto, Rosaria
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p. 3787 - 3794
(2021/10/20)
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- Synthesis and electrochemical polymerization of a novel 2-(thiophen-2-yl)-4-(thiophen-2-ylmethylene)oxazol-5(4H)-one monomer for supercapacitor applications
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In this study, the organic synthesis, electrochemical polymerization and electrochemical characterization of a novel 2-(thiophen-2-yl)-4-(thiophen-2-ylmethylene)oxazol-5(4H)-one, 3, monomer have been reported for supercapacitor applications. Electrode active material was formed electrochemically coating of poly(2-(thiophen-2-yl)-4-(thiophen-2-ylmethylene)oxazol-5(4H)-one) (PTTMO) on pencil graphite electrode (PGE). Electrochemical polymerization was carried out by chronoamperometric (CA) technique in an acetonitrile (ACN) solution containing 0.01 M monomer and 0.10 M tetrabuthylammonium perchlorate (TBAP). The prepared PGE/PTTMO electrode has been monitored by scanning electron microscopy (SEM). Electrochemical properties of the electrode have been investigated by CV, electrochemical impedance spectroscopy (EIS), galvanostatic charge-discharge and repeating chronopotentiometry (RCP) techniques with two or three electrode systems. PGE/PTTMO has exhibited a capacitive performance with highest specific capacitances of 193.00 F g- 1 at a scan rate of 10 mV s- 1. On the other hand, the electrode has shown good charge-discharge cycling stability with the retained ratio about 90.83%.
- Hür, Evrim,Arslan, Anda?,Hür, Deniz
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- Synthesis, biological activity screening and molecular modeling study of acylaminoacetamide derivatives
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In this study, non-rigid analogs of thalidomide have been designed in order to develop potentially active, more effective and safer lead molecules for disorders caused or contributed by inflammation. Five different series of acylaminoacetamide compounds were synthesized, and the biological inhibitory potency of the title compounds has been determined by evaluating their effects on COX-2 isoenzyme expression and PGE2 production in A549 (human lung adenocarcinoma) cell lines. Among the studied series, N-[2-(isopropylamino)-2-oxoethyl]isonicotinamide is the most active inhibitory compound on COX-2 isoenzyme expression, and N-[2-oxo-2-(pyrolydine-1-yl)etyl]isonicotinamide is the most active inhibitory compound on the biosynthesis of PGE2. Molecular docking studies and molecular dynamics simulations were also applied to investigate non-covalent interactions of the most active compounds inside the active side of the crystal structure of murine cyclooxygenase 2 (mCOX-2) isoenzyme.
- Coban, Gunes,Kose, Fadime Aydin,Kirmizibayrak, Petek Ballar,Pabuccuoglu, Varol
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p. 3710 - 3729
(2015/09/07)
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- Novel affinity ligands for chromatography using combinatorial chemistry
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Spatially addressable combinatorial libraries were synthesized by solution phase chemistry and screened for binding to human serum albumin. Members of arylidene diamide libraries were among the best hits found, having submicromolar binding affinities. The results were analyzed by the frequency with which particular substituents appeared among the most potent compounds. After immobilization of the ligands either through the oxazolone or the amine substituent, characterization by surface plasmon resonance showed that ibuprofen affected the binding kinetics, but phenylbutazone did not. It is therefore likely that these compounds bind to Site 2 in sub domain IIIA of human serum albumin (HSA).
- Regberg, Tor,Lindquist, Charlotta,Pilotti, Ake,Ellstroem, Christel,Faegerstam, Lars,Eckersten, Ann,Shinohara, Yasuro,Gallion, Steven L.,Hogan Jr., Joseph C.
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experimental part
p. 267 - 278
(2012/05/05)
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- PYRIMIDINE DERIVATIVES AS POSH AND POSH-AP INHIBITORS
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Pyrimidine derivatives are ubiquitination inhibitors that inhibit the ubiquitin ligase activity, particularly of POSH polypeptides, are useful for the treatment of viral infections and neurological disorders.
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Page/Page column 60-61
(2008/12/05)
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- Cyclocondensation reactions of heterocyclic carbonyl compounds XI [1]. Synthesis and study of cyclocondensation reactions of some 3-substituted-5-(2- aminobenzyl)-1H-[1,2,4]triazine-6-ones
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A series of 2-substituted-4-(2-nitrobenzylidene)-4,5-dihydrooxazol-5-ones (2a-2i) was prepared by the Erlenmeyer's synthesis of 2-nitrobenzaldehyde with acylglycines (1a-1i) and the series of corresponding aminoderivatives (3b-3d and 3g-3i) was synthetise
- Gucky, Tomas,Slouka, Jan,Malon, Michal,Frysova, Iveta
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p. 613 - 621
(2007/10/03)
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