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Journal of Enzyme Inhibition and Medicinal Chemistry

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https://www.readbyqxmd.com/read/27801600/tertiary-amine-derivatives-of-chlorochalcone-as-acetylcholinesterase-ache-and-buthylcholinesterase-buche-inhibitors-the-influence-of-chlorine-alkyl-amine-side-chain-and-%C3%AE-%C3%AE-unsaturated-ketone-group
#1
Xiao-Hui Gao, Chao Zhou, Hao-Ran Liu, Lin-Bo Liu, Jing-Jing Tang, Xin-Hua Xia
A new series of tertiary amine derivatives of chlorochalcone (4a∼4l) were designed, synthesized and evaluated for the effect on acetylcholinesterase (AChE) and buthylcholinesterase (BuChE). The results indicated that all compounds revealed moderate or potent inhibitory activity against AChE, and some possessed high selectivity for AChE over BuChE. The structure-activity investigation showed that the substituted position of chlorine significantly influenced the activity and selectivity. The alteration of tertiary amine group also leads to obvious change in bioactivity...
November 1, 2016: Journal of Enzyme Inhibition and Medicinal Chemistry
https://www.readbyqxmd.com/read/27798977/a-class-of-carbonic-anhydrase-i-selective-activators
#2
Erol Licsandru, Muhammet Tanc, Istvan Kocsis, Mihail Barboiu, Claudiu T Supuran
A series of ureido and bis-ureido derivatives were prepared by reacting histamine with alkyl/aryl-isocyanates or di-isocyanates. The obtained derivatives were assayed as activators of the enzyme carbonic anhydrase (CA, EC 4.2.1.1), due to the fact that histamine itself has this biological activity. Although inhibition of CAs has pharmacological applications in the field of antiglaucoma, anticonvulsant, anticancer, and anti-infective agents, activation of these enzymes is not yet properly exploited pharmacologically for cognitive enhancement or Alzheimer's disease treatment, conditions in which a diminished CA activity was reported...
November 1, 2016: Journal of Enzyme Inhibition and Medicinal Chemistry
https://www.readbyqxmd.com/read/27781494/novel-ffa1-gpr40-agonists-containing-spirocyclic-periphery-polar-azine-periphery-as-a-driver-of-potency
#3
Mikhail Krasavin, Alexey Lukin, Daria Bagnyukova, Nikolay Zhurilo, Ihor Zahanich, Sergey Zozulya
A series of nine compounds based on 3-[4-(benzyloxy)phenyl]propanoic acid core containing a 1-oxa-9-azaspiro[5.5]undecane periphery was designed, synthesized and evaluated as free fatty acid 1 (FFA1 or GPR40) agonists. The spirocyclic appendages included in these compounds were inspired by LY2881835, Eli Lilly's advanced drug candidate for type II diabetes mellitus that was in phase I clinical trials. These polar spirocyclic, fully saturated appendages (that are themselves uncharacteristic of the known FFA1 ligand space) were further decorated with diverse polar groups (such as basic heterocycles or secondary amides)...
October 26, 2016: Journal of Enzyme Inhibition and Medicinal Chemistry
https://www.readbyqxmd.com/read/28102089/disulfiram-moderately-restores-impaired-hepatic-redox-status-of-rats-subchronically-exposed-to-cadmium
#4
Aida Begic, Ana Djuric, Milica Ninkovic, Ivana Stevanovic, Dragan Djurdjevic, Milos Pavlovic, Katarina Jelic, Ana Pantelic, Goran Zebic, Bratislav Dejanovic, Ivan Stanojevic, Danilo Vojvodic, Petar Milosavljevic, Mirjana Djukic, Luciano Saso
Examination of cadmium (Cd) toxicity and disulfiram (DSF) effect on liver was focused on oxidative stress (OS), bioelements status, morphological and functional changes. Male Wistar rats were intraperitoneally treated with 1 mg CdCl2/kg BW/day; orally with 178.5 mg DSF/kg BW/day for 1, 3, 10 and 21 days; and co-exposed from 22nd to 42nd day. The co-exposure nearly restored previously suppressed total superoxide dismutase (SOD), catalase (CAT) and increased glutathione peroxidase (GPx) activities; increased previously reduced glutathione reductase (GR) and total glutathione-S-transferase (GST) activities; reduced previously increased superoxide anion radical (O2(·-)) and malondialdehyde (MDA) levels; increased zinc (Zn) and iron (Fe), and decreased copper (Cu) (yet above control value), while magnesium (Mg) was not affected; and decreased serum alanine aminotransferases (ALT) levels...
December 2017: Journal of Enzyme Inhibition and Medicinal Chemistry
https://www.readbyqxmd.com/read/28100083/%C3%AE-glucosidase-inhibitory-activity-and-cytotoxic-effects-of-some-cyclic-urea-and-carbamate-derivatives
#5
Jelena B Popović-Djordjević, Ivana I Jevtić, Nadja Dj Grozdanić, Sandra B Šegan, Mario V Zlatović, Milovan D Ivanović, Tatjana P Stanojković
The inhibitory activities of selected cyclic urea and carbamate derivatives (1-13) toward α-glucosidase (α-Gls) in in vitro assay were examined in this study. All examined compounds showed higher inhibitory activity (IC50) against α-Gls compared to standard antidiabetic drug acarbose. The most potent was benzyl (3,4,5-trimethoxyphenyl)carbamate (12) with IC50 = 49.85 ± 0.10 µM. In vitro cytotoxicity of the investigated compounds was tested on three human cancer cell lines HeLa, A549 and MDA-MB-453 using MTT assay...
December 2017: Journal of Enzyme Inhibition and Medicinal Chemistry
https://www.readbyqxmd.com/read/28100082/synthesis-and-bioactivity-of-several-new-hetaryl-sulfonamides
#6
Parham Taslimi, Afsun Sujayev, Sevgi Mamedova, Pınar Kalın, İlhami Gulçin, Nastaran Sadeghian, Sukru Beydemir, O Irfan Kufrevioglu, Saleh H Alwasel, Vagif Farzaliyev, Sabir Mamedov
1-(4-Methylsulfonyl)-2-thione-4-aryl-5-Z-6-methyl and oxyalkyl-imidazoles were synthesized from different tetrahydropyrimidinethiones and aryl sulfonyl chloride. These compunds were tested for metal chelating effects and to determine the phrase in which inhibition occured between two physiologically pertinent compunds and carbonic anhydrase (CA) isozymes I and II (hCA I and II), butyrylcholinesterase (BChE) and acetylcholinesterase (AChE). AChE was detected in high concentrations in the brain and red blood cells...
December 2017: Journal of Enzyme Inhibition and Medicinal Chemistry
https://www.readbyqxmd.com/read/28100079/a-novel-proton-transfer-salt-of-2-amino-6-sulfamoylbenzothiazole-and-its-metal-complexes-the-evaluation-of-their-inhibition-effects-on-human-cytosolic-carbonic-anhydrases
#7
Zeynep Alkan Alkaya, Halil İlkimen, Cengiz Yenikaya, Yasemin Kaygısız, Metin Bülbül, Tuncay Tunç, Musa Sarı
A novel proton transfer compound (SMHABT)(+)(HDPC)(-) (1) obtained from 2-amino-6-sulfamoylbenzothiazole (SMABT) and 2,6-pyridinedicarboxylic acid (H2DPC) and its Fe(III), Co(II), Ni(II) complexes (2-4), and Fe(II) complex of SMABT (5) have been prepared and characterized by spectroscopic techniques. Additionally, single crystal X-ray diffraction techniques were applied to complexes (2-4). All complexes (2-4) have distorted octahedral conformations and the structure of 5 might be proposed as octahedral according to spectral and analytical results...
December 2017: Journal of Enzyme Inhibition and Medicinal Chemistry
https://www.readbyqxmd.com/read/28098499/inhibition-of-leishmania-infantum-trypanothione-reductase-by-diaryl-sulfide-derivatives
#8
Francesco Saccoliti, Gabriella Angiulli, Giovanni Pupo, Luca Pescatori, Valentina Noemi Madia, Antonella Messore, Gianni Colotti, Annarita Fiorillo, Luigi Scipione, Marina Gramiccia, Trentina Di Muccio, Roberto Di Santo, Roberta Costi, Andrea Ilari
The study presented here aimed at identifying a new class of compounds acting against Leishmania parasites, the causative agent of Leishmaniasis. For this purpose, the thioether derivatives of our in-house library have been evaluated in whole-cell screening assays in order to determine their in vitro activity against Leishmania protozoan. Among them, promising results have been achieved with compound RDS 777 (6-(sec-butoxy)-2-((3-chlorophenyl)thio)pyrimidin-4-amine) (IC50 = 29.43 µM), which is able to impair the mechanism of the parasite defence against the reactive oxygen species by inhibiting the trypanothione reductase (TR) with high efficiency (Ki 0...
December 2017: Journal of Enzyme Inhibition and Medicinal Chemistry
https://www.readbyqxmd.com/read/28097916/exploring-the-first-rimonabant-analog-opioid-peptide-hybrid-compound-as-bivalent-ligand-for-cb1-and-opioid-receptors
#9
Adriano Mollica, Sveva Pelliccia, Valeria Famiglini, Azzurra Stefanucci, Giorgia Macedonio, Annalisa Chiavaroli, Giustino Orlando, Luigi Brunetti, Claudio Ferrante, Stefano Pieretti, Ettore Novellino, Sandor Benyhe, Ferenc Zador, Anna Erdei, Edina Szucs, Reza Samavati, Szalbolch Dvrorasko, Csaba Tomboly, Rino Ragno, Alexandros Patsilinakos, Romano Silvestri
Cannabinoid (CB) and opioid systems are both involved in analgesia, food intake, mood and behavior. Due to the co-localization of µ-opioid (MOR) and CB1 receptors in various regions of the central nervous system (CNS) and their ability to form heterodimers, bivalent ligands targeting to both these systems may be good candidates to investigate the existence of possible cross-talking or synergistic effects, also at sub-effective doses. In this work, we selected from a small series of new Rimonabant analogs one CB1R reverse agonist to be conjugated to the opioid fragment Tyr-D-Ala-Gly-Phe-NH2...
December 2017: Journal of Enzyme Inhibition and Medicinal Chemistry
https://www.readbyqxmd.com/read/28097912/methanethiosulfonate-derivatives-as-ligands-of-the-stat3-sh2-domain
#10
Elena Gabriele, Chiara Ricci, Fiorella Meneghetti, Nicola Ferri, Akira Asai, Anna Sparatore
With the aim to discover new STAT3 direct inhibitors, potentially useful as anticancer agents, a set of methanethiosulfonate drug hybrids were synthesized. The in vitro tests showed that all the thiosulfonic compounds were able to strongly and selectively bind STAT3-SH2 domain, whereas the parent drugs were completely devoid of this ability. In addition, some of them showed a moderate antiproliferative activity on HCT-116 cancer cell line. These results suggest that methanethiosulfonate moiety can be considered a useful scaffold in the preparation of new direct STAT3 inhibitors...
December 2017: Journal of Enzyme Inhibition and Medicinal Chemistry
https://www.readbyqxmd.com/read/28097911/design-synthesis-and-docking-study-of-novel-coumarin-ligands-as-potential-selective-acetylcholinesterase-inhibitors
#11
Fatih Sonmez, Belma Zengin Kurt, Isil Gazioglu, Livia Basile, Aydan Dag, Valentina Cappello, Tiziana Ginex, Mustafa Kucukislamoglu, Salvatore Guccione
New coumaryl-thiazole derivatives with the acetamide moiety as a linker between the alkyl chains and/or the heterocycle nucleus were synthesized and in vitro tested as acetylcholinesterase (AChE) inhibitors. 2-(diethylamino)-N-(4-(2-oxo-2H-chromen-3-yl)thiazol-2-yl)acetamide (6c, IC50 value of 43 nM) was the best AChE inhibitor with a selectivity index of 4151.16 over BuChE. Kinetic study of AChE inhibition revealed that 6c was a mixed-type inhibitor. Moreover, the result of H4IIE hepatoma cell toxicity assay for 6c showed negligible cell death...
December 2017: Journal of Enzyme Inhibition and Medicinal Chemistry
https://www.readbyqxmd.com/read/28097910/purification-and-biochemical-characterization-of-a-novel-thermostable-serine-alkaline-protease-from-aeribacillus-pallidus-c10-a-potential-additive-for-detergents
#12
Vildan Yildirim, Mustafa Ozkan Baltaci, Ilknur Ozgencli, Melda Sisecioglu, Ahmet Adiguzel, Gulsah Adiguzel
An extracellular thermostable alkaline serine protease enzyme from Aeribacillus pallidus C10 (GenBank No: KC333049), was purified 4.85 and 17. 32-fold with a yield of 26.9 and 19.56%, respectively, through DE52 anion exchange and Probond affinity chromatography. The molecular mass of the enzyme was determined through sodium dodecyl sulfate-polyacrylamide gel electrophoresis (SDS-PAGE), with approximately 38.35 kDa. The enzyme exhibited optimum activity at pH 9 and at temperature 60 °C. It was determined that the enzyme had remained stable at the range of pH 7...
December 2017: Journal of Enzyme Inhibition and Medicinal Chemistry
https://www.readbyqxmd.com/read/28097907/the-lignicolous-fungus-trametes-versicolor-l-lloyd-1920-a-promising-natural-source-of-antiradical-and-ache-inhibitory-agents
#13
Ljiljana Janjušević, Maja Karaman, Filip Šibul, Giuseppina Tommonaro, Carmine Iodice, Dragica Jakovljević, Boris Pejin
This study aimed to determine antiradical (DPPH(•) and (•)OH) and acetylcholinesterase (AChE) inhibitory activities along with chemical composition of autochtonous fungal species Trametes versicolor (Serbia). A total of 38 phenolic compounds with notable presence of phenolic acids were identified using HPLC/MS-MS. Its water extract exhibited the highest antiradical activity against (•)OH (3.21 μg/mL), among the rest due to the presence of gallic, p-coumaric and caffeic acids. At the concentration of 100 μg/mL, the same extract displayed a profound AChE inhibitory activity (60...
December 2017: Journal of Enzyme Inhibition and Medicinal Chemistry
https://www.readbyqxmd.com/read/28097906/synthesis-of-new-pyridothienopyrimidinone-derivatives-as-pim-1-inhibitors
#14
Bassem H Naguib, Hala B El-Nassan, Tamer M Abdelghany
Four series of pyridothienopyrimidin-4-one derivatives were designed and prepared to improve the pim-1 inhibitory activity of the previously reported thieno[2,3-b]pyridines. Significant improvement in the pim-1 inhibition and cytotoxic activity was achieved using structure rigidification strategy via ring closure. Six compounds (6c, 7a, 7c, 7d, 8b and 9) showed highly potent pim-1 inhibitory activity with IC50 of 4.62, 1.18, 1.38, 1.97, 8.83 and 4.18 μM, respectively. Four other compounds (6b, 6d, 7b and 8a) showed moderate pim-1 inhibition...
December 2017: Journal of Enzyme Inhibition and Medicinal Chemistry
https://www.readbyqxmd.com/read/28097905/discovery-of-novel-dual-inhibitors-of-receptor-tyrosine-kinases-egfr-and-igf-1r
#15
Cornelius Hempel, Frank Totzke, Christoph Schächtele, Abdulkarim Najjar, Wolfgang Sippl, Christoph Ritter, Andreas Hilgeroth
Novel 4-benzylamino benzo-anellated pyrrolo[2,3-b]pyridines have been synthesized with varied substitution patterns both at the molecular scaffold of the benzo-anellated ring and at the 4-benzylamino residue. With a structural similarity to substituted thieno[2,3-d]pyrimidines as epidermal growth factor receptor (EGFR) inhibitors, we characterized the inhibition of EGFR for our novel compounds. As receptor heterodimerization gained certain interest as mechanism of cancer cells to become resistant against novel protein kinase inhibitors, we additionally measured the inhibition of insulin-like growth factor receptor IGF-1R which is a prominent receptor for such heterodimerizations with EGFR...
December 2017: Journal of Enzyme Inhibition and Medicinal Chemistry
https://www.readbyqxmd.com/read/28097901/skin-whitening-agents-medicinal-chemistry-perspective-of-tyrosinase-inhibitors
#16
Thanigaimalai Pillaiyar, Manoj Manickam, Vigneshwaran Namasivayam
Melanogenesis is a process to synthesize melanin, which is a primary responsible for the pigmentation of human skin, eye and hair. Although numerous enzymatic catalyzed and chemical reactions are involved in melanogenesis process, the enzymes such as tyrosinase and tyrosinase-related protein-1 (TRP-1) and TRP-2 played a major role in melanin synthesis. Specifically, tyrosinase is a key enzyme, which catalyzes a rate-limiting step of the melanin synthesis, and the downregulation of tyrosinase is the most prominent approach for the development of melanogenesis inhibitors...
December 2017: Journal of Enzyme Inhibition and Medicinal Chemistry
https://www.readbyqxmd.com/read/28097900/structure-activity-relationships-of-fraxamoside-as-an-unusual-xanthine-oxidase-inhibitor
#17
Rosa Maria Vitale, Lina Antenucci, Margherita Gavagnin, Gennaro Raimo, Pietro Amodeo
Fraxamoside, a macrocyclic secoiridoid glucoside featuring a hydroxytyrosol group, was recently identified as a xanthine oxidase inhibitor (XOI) comparable in potency in vitro to the standard antigout drug allopurinol. However, this activity and its considerably higher value than its derivatives oleuropein, oleoside 11-methyl ester, and hydroxytyrosol are not explained by structure-activity relationships (SARs) of known XOIs. To exclude allosteric mechanisms, we first determined the inhibition kinetic of fraxamoside...
December 2017: Journal of Enzyme Inhibition and Medicinal Chemistry
https://www.readbyqxmd.com/read/28097898/two-approaches-to-the-use-of-benzo-c-1-2-oxaboroles-as-active-fragments-for-synthetic-transformation-of-clarithromycin
#18
Gennady B Lapa, Elena P Mirchink, Elena B Isakova, Maria N Preobrazhenskaya
Clarithromycin (active against Gram positive infections) and 1-hydroxy-1,3-dihydrobenzo[c][1,2]oxaborole derivatives (effective for Gram negative microbes) are the ligands of bacterial RNA. The antimicrobial activities of these benzoxaboroles linked with clarithromycin at 9 or 4″ position were compared. Two synthetic pathways for these conjugates were elaborated. First pathway explored the substitution of the C-9 carbonyl group of macrolactone's cycle via oxime linker, the second direction used the modification of the 4″-O-group of cladinose via the formation of carbamates of benzoxaboroles...
December 2017: Journal of Enzyme Inhibition and Medicinal Chemistry
https://www.readbyqxmd.com/read/28097897/carbonic-anhydrase-inhibitory-properties-of-some-uracil-derivatives
#19
Emir Alper Türkoğlu, Murat Şentürk, Claudiu T Supuran, Deniz Ekinci
Inhibitors of carbonic anhydrase (CA) have been carried out in many therapeutic applications, especially antiglaucoma activity. In this study, we investigated some uracil derivatives (4-12) to inhibit human CA I (hCA I) and II (hCA II) isoenzymes. The KI values of the compounds 4-12 are in the range of 0.085-428 µM for hCA I and of 0.1715-645 µM against hCA II, respectively. It is concluded from the kinetic investigations, all compounds used in the study act as competitive inhibitors with substrate, 4-NPA...
December 2017: Journal of Enzyme Inhibition and Medicinal Chemistry
https://www.readbyqxmd.com/read/28097896/a-new-nitrobenzoxadiazole-based-gstp1-1-inhibitor-with-a-previously-unheard-of-mechanism-of-action-and-high-stability
#20
Chiara Fulci, Dante Rotili, Anastasia De Luca, Lorenzo Stella, Blasco Morozzo Della Rocca, Mariantonietta Forgione, Veronica Di Paolo, Antonello Mai, Mattia Falconi, Luigi Quintieri, Anna M Caccuri
CONTEXT: The nitrobezoxadiazole derivative NBDHEX is a potent inhibitor of glutathione transferase P1-1 (GSTP1-1) endowed with outstanding anticancer activity in different tumor models. OBJECTIVE: To characterize by in vitro biochemical and in silico studies the NBDHEX analogues named MC2752 and MC2753. MATERIALS AND METHODS: Synthesis of MC2752 and MC2753, biochemical assays and in silico docking and normal-mode analyses. RESULTS: The presence of a hydrophobic moiety in the side chain of MC2753 confers unique features to this molecule...
December 2017: Journal of Enzyme Inhibition and Medicinal Chemistry
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