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Journal of Enzyme Inhibition and Medicinal Chemistry

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https://www.readbyqxmd.com/read/28965424/neem-oil-nanoemulsions-characterisation-and-antioxidant-activity
#1
Federica Rinaldi, Patrizia Nadia Hanieh, Catia Longhi, Simone Carradori, Daniela Secci, Gokhan Zengin, Maria Grazia Ammendolia, Elena Mattia, Elena Del Favero, Carlotta Marianecci, Maria Carafa
The aim of the present work is to develop nanoemulsions (NEs), nanosized emulsions, manufactured for improving the delivery of active pharmaceutical ingredients. In particular, nanoemulsions composed of Neem seed oil, contain rich bioactive components, and Tween 20 as nonionic surfactant were prepared. A mean droplet size ranging from 10 to 100 nm was obtained by modulating the oil/surfactant ratio. Physicochemical characterisation was carried out evaluating size, ζ-potential, microviscosity, polarity and turbidity of the external shell and morphology, along with stability in simulated cerebrospinal fluid (CSF), activity of Neem oil alone and in NEs, HEp-2 cell interaction and cytotoxicity studies...
December 2017: Journal of Enzyme Inhibition and Medicinal Chemistry
https://www.readbyqxmd.com/read/28965419/discovery-of-curcumin-inspired-sulfonamide-derivatives-as-a-new-class-of-carbonic-anhydrase-isoforms-i-ii-ix-and-xii-inhibitors
#2
P V Sri Ramya, Srinivas Angapelly, Andrea Angeli, Chander Singh Digwal, Mohammed Arifuddin, Bathini Nagendra Babu, Claudiu T Supuran, Ahmed Kamal
A series of curcumin inspired sulfonamide derivatives was prepared from various chalcones and 4-sulfamoyl benzaldehyde via Claisen-Schmidt condensation. All new compounds were assayed as inhibitors of four human isoforms of the metalloenzyme carbonic anhydrase (hCA, EC 4.2.1.1) isoforms hCA I, II, IX and XII. Interesting inhibitory activities were observed against all these isoforms. hCA I, an isoform involved in several eye diseases was inhibited moderately with KIs in the range of 191.8-904.2 nM, hCA II, an antiglaucoma drug target was highly inhibited by the new sulfonamides, with KIs in the range of 0...
December 2017: Journal of Enzyme Inhibition and Medicinal Chemistry
https://www.readbyqxmd.com/read/28948845/dual-targeting-of-cancer-related-human-matrix-metalloproteinases-and-carbonic-anhydrases-by-chiral-n-biarylsulfonyl-phosphonic-acids
#3
Grazia Luisi, Guido Angelini, Carla Gasbarri, Antonio Laghezza, Mariangela Agamennone, Fulvio Loiodice, Claudiu T Supuran, Cristina Campestre, Paolo Tortorella
A series of nanomolar phosphonate matrix metalloproteinase (MPP) inhibitors was tested for inhibitory activity against a panel of selected human carbonic anhydrase (CA, EC 4.2.1.1) isozymes, covering the cancer-associated CA IX and XII. None of the reported sulfonyl and sulfonylamino-derivatives sensitively affected the catalytic activity of the cytosolic isoforms CA I and II, which are considered off-target isoforms in view of their physiological role. The most active inhibitors were in the series of chiral N-(sulfonyl)phosphovaline derivatives, which showed good to excellent inhibitory activity over target CAs, with compound 15 presenting the best isoform-selectivity toward CA IX...
December 2017: Journal of Enzyme Inhibition and Medicinal Chemistry
https://www.readbyqxmd.com/read/28948843/synthesis-in-vitro-antitumour-activity-and-molecular-docking-study-of-novel-2-substituted-mercapto-3-3-4-5-trimethoxybenzyl-4-3h-quinazolinone-analogues
#4
Adel S El-Azab, Alaa A-M Abdel-Aziz, Hazem A Ghabbour, Manal A Al-Gendy
A novel series of 2-substituted mercapto-3-(3,4,5-trimethoxybenzyl)-4(3H)-quinazolinones 1-20 was synthesised and evaluated for in vitro antitumour activity. N-(4-Chlorophenyl)-2-[(3-(3,4,5-trimethoxybenzyl)-4(3H)-quinazolinon-2-yl)thio)acetamide (7) and N-(3,4,5 trimethoxybenzyl)-2-[(3-(3,4,5-trimethoxybenzyl)-4(3H)-quinazolinon-2-yl)thio]propanamide (19) exhibited excellent antitumour properties, with mean growth inhibitory concentration (GI50) of 17.90 and 6.33 µΜ, respectively, compared with those of 5-fluorouracil 5-FU, gefitinib, and erlotinib (mean GI50: 18...
December 2017: Journal of Enzyme Inhibition and Medicinal Chemistry
https://www.readbyqxmd.com/read/28936885/psychoactive-substances-belonging-to-the-amphetamine-class-potently-activate-brain-carbonic-anhydrase-isoforms-va-vb-vii-and-xii
#5
Andrea Angeli, Fabio Vaiano, Francesco Mari, Elisabetta Bertol, Claudiu T Supuran
Identifying possible new biological activities of psychoactive substances belonging to various chemical classes may lead to a better understanding of their mode of action and side effects. We report here that amines structurally related to amphetamine, a widely used psychoactive substance, such as amphetamine, methamphetamine, phentermine, mephentermine, and chlorphenteramine, potently activate several carbonic anhydrase (CA, EC 4.2.1.1) isoforms involved in important physiological functions. Of the 11 investigated human (h) isoforms, the widespread hCA I and II, the secreted hCA VI, as well as the cytosolic hCA XIII, and membrane-bound hCA IX and XIV were poorly activated by these amines, whereas the extracellular hCA IV, the mitochondrial enzymes hCA VA/VB, the cytosolic hCA VII, and the transmembrane isoform hCA XII were potently activated...
December 2017: Journal of Enzyme Inhibition and Medicinal Chemistry
https://www.readbyqxmd.com/read/28936880/development-of-terphenyl-2-methyloxazol-5-4h-one-derivatives-as-selective-reversible-magl-inhibitors
#6
Carlotta Granchi, Isabella Caligiuri, Eleonora Bertelli, Giulio Poli, Flavio Rizzolio, Marco Macchia, Adriano Martinelli, Filippo Minutolo, Tiziano Tuccinardi
Monoacylglycerol lipase is a serine hydrolase that plays a major role in the degradation of the endocannabinoid neurotransmitter 2-arachidonoylglycerol. A wide number of MAGL inhibitors are reported in literature; however, many of them are characterised by an irreversible mechanism of action and this behavior determines an unwanted chronic MAGL inactivation, which acquires a functional antagonism of the endocannabinoid system. The possible use of reversible MAGL inhibitors has only recently been explored, due to the lack of known compounds possessing efficient reversible inhibitory activities...
December 2017: Journal of Enzyme Inhibition and Medicinal Chemistry
https://www.readbyqxmd.com/read/28933564/%C3%AE-glucosidase-inhibition-by-flavonoids-an-in-vitro-and-in-silico-structure-activity-relationship-study
#7
Carina Proença, Marisa Freitas, Daniela Ribeiro, Eduardo F T Oliveira, Joana L C Sousa, Sara M Tomé, Maria J Ramos, Artur M S Silva, Pedro A Fernandes, Eduarda Fernandes
α-Glucosidase inhibitors are described as the most effective in reducing post-prandial hyperglycaemia (PPHG) from all available anti-diabetic drugs used in the management of type 2 diabetes mellitus. As flavonoids are promising modulators of this enzyme's activity, a panel of 44 flavonoids, organised in five groups, was screened for their inhibitory activity of α-glucosidase, based on in vitro structure-activity relationship studies. Inhibitory kinetic analysis and molecular docking calculations were also applied for selected compounds...
December 2017: Journal of Enzyme Inhibition and Medicinal Chemistry
https://www.readbyqxmd.com/read/28933241/characterization-of-human-s-adenosyl-homocysteine-hydrolase-in-vitro-and-identification-of-its-potential-inhibitors
#8
Weiwei Hao, Yanhua Li, Qiuli Shan, Tian Han, Wencheng Li, Sheng He, Kongkai Zhu, Yumei Li, Xiaojun Tan, Jinsong Gu
Human S-adenosyl-homocysteine hydrolase (SAHH, E.C.3.3.1.1) has been considered to be an attractive target for the design of medicines to treat human disease, because of its important role in regulating biological methylation reactions to catalyse the reversible hydrolysis of S-adenosylhomocysteine (SAH) to adenosine (Ado) and l-homocysteine (Hcy). In this study, SAHH protein was successfully cloned and purified with optimized, Pichia pastoris (P. pastoris) expression system. The biological activity results revealed that, among the tested compounds screened by ChemMapper and SciFinder Scholar, 4-(3-hydroxyprop-1-en-1-yl)-2-methoxyphenol (coniferyl alcohol, CAS: 458-35-5, ZINC: 12359045) exhibited the highest inhibition against rSAHH (IC50= 34 nM)...
December 2017: Journal of Enzyme Inhibition and Medicinal Chemistry
https://www.readbyqxmd.com/read/28933232/reactive-oxygen-species-inhibit-catalytic-activity-of-peptidylarginine-deiminase
#9
Dres Damgaard, Mads Emil Bjørn, Peter Østrup Jensen, Claus Henrik Nielsen
Protein citrullination catalysed by peptidylarginine deiminase (PAD) may play an important pathogenic role in several chronic inflammatory diseases and malignancies. PAD2, PAD4, and citrullinated proteins are found in the synovium of rheumatoid arthritis patients. PAD activity is dependent on calcium and reducing conditions. However, reactive oxygen species (ROS) have been shown to induce citrullination of histones in granulocytes. Here we examine the ability of H2O2 and leukocyte-derived ROS to regulate PAD activity using citrullination of fibrinogen as read-out...
December 2017: Journal of Enzyme Inhibition and Medicinal Chemistry
https://www.readbyqxmd.com/read/28933230/inhibition-of-protein-tyrosine-phosphatase-ptp1b-and-%C3%AE-glucosidase-by-geranylated-flavonoids-from-paulownia-tomentosa
#10
Yeong Hun Song, Zia Uddin, Young Min Jin, Zuopeng Li, Marcus John Curtis-Long, Kwang Dong Kim, Jung Keun Cho, Ki Hun Park
Protein tyrosine phosphatase 1B (PTP1B) and α-glucosidase are important targets to treat obesity and diabetes, due to their deep correlation with insulin and leptin signalling, and glucose regulation. The methanol extract of Paulownia tomentosa fruits showed potent inhibition against both enzymes. Purification of this extract led to eight geranylated flavonoids (1-8) displaying dual inhibition of PTP1B and α-glucosidase. The isolated compounds were identified as flavanones (1-5) and dihydroflavonols (6-8)...
December 2017: Journal of Enzyme Inhibition and Medicinal Chemistry
https://www.readbyqxmd.com/read/28891347/synthesis-and-biological-evaluation-of-aminomethyl-and-alkoxymethyl-derivatives-as-carbonic-anhydrase-acetylcholinesterase-and-butyrylcholinesterase-inhibitors
#11
İlhami Gulçin, Malahat Abbasova, Parham Taslimi, Zübeyir Huyut, Leyla Safarova, Afsun Sujayev, Vagif Farzaliyev, Şükrü Beydemir, Saleh H Alwasel, Claudiu T Supuran
Compounds containing nitrogen and sulfur atoms can be widely used in various fields such as industry, medicine, biotechnology and chemical technology. Therefore, the reactions of aminomethylation and alkoxymethylation of mercaptobenzothiazole, mercaptobenzoxazole and 2-aminothiazole were developed. Additionally, the alkoxymethyl derivatives of mercaptobenzoxazole and 2-aminothiazole were synthesized by a reaction with hemiformals, which are prepared by the reaction of alcohols and formaldehyde. In this study, the inhibitory effects of these molecules were investigated against acetylcholinesterase (AChE), butyrylcholinesterase (BChE) enzymes and carbonic anhydrase I, and II isoenzymes (hCA I and II)...
December 2017: Journal of Enzyme Inhibition and Medicinal Chemistry
https://www.readbyqxmd.com/read/28891338/synthesis-and-biological-evaluation-of-benzenesulphonamide-bearing-1-4-5-trisubstituted-1-2-3-triazoles-possessing-human-carbonic-anhydrase-i-ii-iv-and-ix-inhibitory-activity
#12
Rajiv Kumar, Vikas Sharma, Silvia Bua, Claudiu T Supuran, Pawan K Sharma
A library of benzenesulphonamides incorporating 1,2,3-triazole rings functionalised with ester, carboxylic acid, carboxamide, carboxyhydrazide, and hydroxymethyl moieties were synthesised. The carbonic anhydrase (CAs, EC 4.2.1.1) inhibitory activity of the new compounds was assessed against four human (h) isoforms, hCA I, hCA II, hCA IV, and hCA IX. Among them, hCA II and IV are anti-glaucoma drug targets, being involved in aqueous humour secretion within the eye. hCA I was inhibited with Ki's ranging between 8...
December 2017: Journal of Enzyme Inhibition and Medicinal Chemistry
https://www.readbyqxmd.com/read/28870094/design-synthesis-and-biological-activity-of-pyrazinamide-derivatives-for-anti-mycobacterium-tuberculosis
#13
Shiyang Zhou, Shanbin Yang, Gangliang Huang
A total of 11 pyrazinamide derivatives were designed and synthesised using pyrazinamide as the lead compound, which was optimised by structural modification with alkyl chains, six-membered rings, and bioisosterism, respectively. The target compounds were synthesised using pyrazinecarboxylic acid as the starting material by acylation, amidation, and alkylation, respectively. Their structures were confirmed by (1)H NMR, (13)C NMR, HRESIMS, and elemental analysis, respectively. The bioactivities of derivatives were assayed using bacteriostatic experiment and minimum inhibitory concentration experiment...
December 2017: Journal of Enzyme Inhibition and Medicinal Chemistry
https://www.readbyqxmd.com/read/28870093/novel-series-of-1-2-4-trioxane-derivatives-as-antimalarial-agents
#14
Mithun Rudrapal, Dipak Chetia, Vineeta Singh
Among three series of 1,2,4-trioxane derivatives, five compounds showed good in vitro antimalarial activity, three compounds of which exhibited better activity against P. falciparum resistant (RKL9) strain than the sensitive (3D7) one. Two best compounds were one from aryl series and the other from heteroaryl series with IC50 values of 1.24 µM and 1.24 µM and 1.06 µM and 1.17 µM, against sensitive and resistant strains, respectively. Further, trioxane derivatives exhibited good binding affinity for the P...
December 2017: Journal of Enzyme Inhibition and Medicinal Chemistry
https://www.readbyqxmd.com/read/28868930/multicomponent-synthesis-of-some-new-1s-4s-2-5-diazabicyclo-2-2-1-heptane-dithiocarbamates-and-their-in-vitro-anti-proliferative-activity-against-caski-mda-mb-231-and-sk-lu-1-tumour-cells-as-apoptosis-inducing-agents-without-necrosis
#15
Sujay Laskar, Luis Sánchez-Sánchez, Manuel López-Ortiz, Hugo López-Muñoz, María L Escobar-Sánchez, Arturo T Sánchez, Ignacio Regla
Identification of a new class of antitumor agent capable to induce apoptosis without triggering necrotic cell death event is challenging. The present communication describes the multicomponent synthesis of seven new (1S,4S)-2,5-diazabicyclo[2.2.1]heptane-dithiocarbamates and their in vitro antiproliferative activity on cervical cancer cell line (CaSki), breast cancer cell line (MDA-MB231), lung cancer cell line (SK-Lu-1) and human lymphocytes. Among the synthesized dithiocarbamates, compound 9e displayed significant antiproliferative activity without inducing any necrotic cell death (both on tumour cells and lymphocytes) and induced apoptosis in tumor cells by the caspase dependent apoptotic pathway...
December 2017: Journal of Enzyme Inhibition and Medicinal Chemistry
https://www.readbyqxmd.com/read/28856944/inhibition-of-human-cytochromes-p450-2a6-and-2a13-by-flavonoids-acetylenic-thiophenes-and-sesquiterpene-lactones-from-pluchea-indica-and-vernonia-cinerea
#16
Supattra Boonruang, Khanistha Prakobsri, Phisit Pouyfung, Ekaruth Srisook, Aruna Prasopthum, Pornpimol Rongnoparut, Songklod Sarapusit
The human liver cytochrome P450 (CYP) 2A6 and the respiratory CYP2A13 enzymes play role in nicotine metabolism and activation of tobacco-specific nitrosamine carcinogens. Inhibition of both enzymes could offer a strategy for smoking abstinence and decreased risks of respiratory diseases and lung cancer. In this study, activity-guided isolation identified four flavonoids 1-4 (apigenin, luteolin, chrysoeriol, quercetin) from Vernonia cinerea and Pluchea indica, four hirsutinolide-type sesquiterpene lactones 5-8 from V...
December 2017: Journal of Enzyme Inhibition and Medicinal Chemistry
https://www.readbyqxmd.com/read/28856935/the-use-of-dimethylsulfoxide-as-a-solvent-in-enzyme-inhibition-studies-the-case-of-aldose-reductase
#17
Livia Misuri, Mario Cappiello, Francesco Balestri, Roberta Moschini, Vito Barracco, Umberto Mura, Antonella Del-Corso
Aldose reductase (AR) is an enzyme devoted to cell detoxification and at the same time is strongly involved in the aetiology of secondary diabetic complications and the amplification of inflammatory phenomena. AR is subjected to intense inhibition studies and dimethyl sulfoxide (DMSO) is often present in the assay mixture to keep the inhibitors in solution. DMSO was revealed to act as a weak but well detectable AR differential inhibitor, acting as a competitive inhibitor of the L-idose reduction, as a mixed type of non-competitive inhibitor of HNE reduction and being inactive towards 3-glutathionyl-4-hydroxynonanal transformation...
December 2017: Journal of Enzyme Inhibition and Medicinal Chemistry
https://www.readbyqxmd.com/read/28856929/new-quinoxalinone-inhibitors-targeting-secreted-phospholipase-a2-and-%C3%AE-glucosidase
#18
Fatmah A S Alasmary, Fatima S Alnahdi, Abir Ben Bacha, Amr M El-Araby, Nadine Moubayed, Ahmed M Alafeefy, Moustafa E El-Araby
Elevated blood glucose and increased activities of secreted phospholipase A2 (sPLA2) are strongly linked to coronary heart disease. In this report, our goal was to develop small heterocyclic compound that inhibit sPLA2. The title compounds were also tested against α-glucosidase and α-amylase. This array of enzymes was selected due to their implication in blood glucose regulation and diabetic cardiovascular complications. Therefore, two distinct series of quinoxalinone derivatives were synthesised; 3-[N'-(substituted-benzylidene)-hydrazino]-1H-quinoxalin-2-ones 3a-f and 1-(substituted-phenyl)-5H-[1,2,4]triazolo[4,3-a]quinoxalin-4-ones 4a-f...
December 2017: Journal of Enzyme Inhibition and Medicinal Chemistry
https://www.readbyqxmd.com/read/28791908/synthesis-and-biological-evaluation-of-novel-7-hydroxy-4-phenylchromen-2-one-linked-to-triazole-moieties-as-potent-cytotoxic-agents
#19
Chuan-Feng Liu, Qing-Kun Shen, Jia-Jun Li, Yu-Shun Tian, Zheshan Quan
A new series of novel 7-hydroxy-4-phenylchromen-2-one (1a)-linked 1,2,4-triazoles were synthesised using a click chemistry approach. All derivatives were subjected to 3-(4,5-dimethylthiazol-yl)-diphenyl tetrazolium bromide (MTT) cytotoxicity screening against a panel of six different human cancer cell lines (AGS, MGC-803, HCT-116, A-549, HepG2, and HeLa) to assess their cytotoxic potential. Among the tested molecules, some of the analogues showed better cytotoxic activity than that shown by the 7-hydroxy-4-phenylchromen-2-one (1a)...
December 2017: Journal of Enzyme Inhibition and Medicinal Chemistry
https://www.readbyqxmd.com/read/28791907/a-one-step-procedure-for-immobilising-the-thermostable-carbonic-anhydrase-sspca-on-the-surface-membrane-of-escherichia-coli
#20
Sonia Del Prete, Rosa Perfetto, Mosè Rossi, Fatmah A S Alasmary, Sameh M Osman, Zeid AlOthman, Claudiu T Supuran, Clemente Capasso
The carbonic anhydrase superfamily (CA, EC 4.2.1.1) of metalloenzymes is present in all three domains of life (Eubacteria, Archaea, and Eukarya), being an interesting example of convergent/divergent evolution, with its seven families (α-, β-, γ-, δ-, ζ-, η-, and θ-CAs) described so far. CAs catalyse the simple, but physiologically crucial reaction of carbon dioxide hydration to bicarbonate and protons. Recently, our groups characterised the α-CA from the thermophilic bacterium, Sulfurihydrogenibium yellowstonense finding a very high catalytic activity for the CO2 hydration reaction (kcat = 9...
December 2017: Journal of Enzyme Inhibition and Medicinal Chemistry
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