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Journal of Enzyme Inhibition and Medicinal Chemistry

Zeynep Soyer, Sirin Uysal, Sulunay Parlar, Ayse Hande Tarikogullari Dogan, Vildan Alptuzun
A series of 4-phthalimidobenzenesulfonamide derivatives were designed, synthesized and evaluated for the inhibitory activities against acetylcholinesterase (AChE) and butyrylcholinesterase (BuChE). Structures of the title compounds were confirmed by spectral and elemental analyses. The cholinesterase (ChE) inhibitory activity studies were carried out using Ellman's colorimetric method. The biological activity results revealed that all of the title compounds (except for compound 8) displayed high selectivity against AChE...
October 21, 2016: Journal of Enzyme Inhibition and Medicinal Chemistry
Nadia G Kandile, Mansoura I Mohamed, Hind M Ismaeel
New compounds based on oxindole moiety were synthesized via the reaction of 5-substitued isatins 1a-e with different nucleophiles such as benzidine, 3,3'-dimethoxybenzidine 2a,b and 2,6-diaminopyridine 3 to afford three different classes of bis-Schiff bases 4a-e, 5a-e and 6a-e, respectively. The structures of the new compounds were elucidated on the basis of their FTIR, (1)H NMR, (13)C NMR, GC/MS spectral data and elemental analysis. The in vitro antimicrobial activity of the new compounds was evaluated using a broth dilution technique in terms of minimal inhibitory concentration (MIC) against four bacterial and two fungal pathogens and anticancer activities against HELA cervix...
October 21, 2016: Journal of Enzyme Inhibition and Medicinal Chemistry
Alessandro Rubini, Vincenzo Catena, Daniele Del Monte, Gerardo Bosco
CONTEXT: Calcium channel blockers may theoretically exhibit relaxing effects not only on vascular smooth muscle but also on airway smooth muscle. OBJECTIVE: To investigate possible effects of nifedipine on respiratory mechanics in the rat. METHODS: Respiratory system mechanical parameters were measured by the end-inflation occlusion method in the rat in vivo before and after the intraperitoneal administration of nifedipine. RESULTS: We found that nifedipine affects respiratory mechanics, inducing a reduction of airway resistance and of respiratory system elastance, probably because of a relaxing action on airway and parenchimal smooth muscle cells...
October 21, 2016: Journal of Enzyme Inhibition and Medicinal Chemistry
Nahid Alimoradi, Mohammad Reza Ashrafi-Kooshk, Mohsen Shahlaei, Shabnam Maghsoudi, Hadi Adibi, Ross P McGeary, Reza Khodarahmi
Purple acid phosphatases (PAPs) are binuclear metallo-hydrolases that have been isolated from various mammals, plants, fungi and bacteria. In mammals, PAP activity is associated with bone resorption and can lead to bone metabolic disorders such as osteoporosis; thus human PAP is an attractive target to develop anti-osteoporotic drugs. The aim of the present study was to investigate inhibitory effect of synthesized diethylalkylsulfonamido(4-methoxyphenyl)methyl)phosphonate/phosphonic acid derivatives as potential red kidney bean PAP (rkbPAP) inhibitors accompanied by experimental and molecular modeling assessments...
October 21, 2016: Journal of Enzyme Inhibition and Medicinal Chemistry
Daria M Monti, Giuseppina De Simone, Emma Langella, Claudiu T Supuran, Anna Di Fiore, Simona M Monti
Carbonic anhydrases (CAs) III and VII are two cytosolic isoforms of the α-CA family which catalyze the physiological reaction of carbon dioxide hydration to bicarbonate and proton. Despite these two enzymes share a 49% sequence identity and present a very similar three-dimensional structure, they show profound differences when comparing the specific activity for CO2 hydration reaction, with CA VII being much more active than CA III. Recently, CA III and CA VII have been proposed to play a new role as scavenger enzymes in cells where oxidative damage occurs...
October 21, 2016: Journal of Enzyme Inhibition and Medicinal Chemistry
Rita Meleddu, Simona Distinto, Angela Corona, Enzo Tramontano, Giulia Bianco, Claudia Melis, Filippo Cottiglia, Elias Maccioni
A series of 3-3-{2-[2-3-methyl-4-phenyl-2,3-dihydro-1,3-thiazol-2-ylidene]hydrazin-1-ylidene-2,3-dihydro-1H-indol-2-one derivatives has been designed and synthesized to study their activity on both HIV-1 (Human Immunodeficiency Virus type 1) RT (Reverse Transcriptase) associated functions. These derivatives are analogs of previously reported series whose biological activity and mode of action have been investigated. In this work we investigated the influence of the introduction of a methyl group in the position 3 of the dihydrothiazole ring and of a chlorine atom in the position 5 of the isatin nucleus...
October 21, 2016: Journal of Enzyme Inhibition and Medicinal Chemistry
Shakeela Yasmeen, Sajjad Hussain Sumrra, Muhammad Safwan Akram, Zahid H Chohan
A novel series of thiophene derived Schiff bases and their transition metal- [Co(II), Cu(II), Zn(II), Ni(II)] based compounds are reported. The Schiff bases act as tridentate ligands toward metal ions via azomethine-N, deprotonated-N of ammine substituents and S-atom of thienyl moiety. The synthesized ligands along with their metal complexes were screened for their in vitro antibacterial activity against six bacterial pathogens (Escherichia coli, Shigella flexneri, Pseudomonas aeruginosa, Salmonella typhi, Staphylococcus aureus and Bacillus subtilis) and for antifungal activity against six fungal pathogens (Trichophytonlongifusus, Candida albicans, Aspergillus flavus, Microsporum canis, Fusarium solani and Candida glabrata)...
October 21, 2016: Journal of Enzyme Inhibition and Medicinal Chemistry
Shaher Bano Mirza, Ramin Ekhteiari Salmas, M Qaiser Fatmi, Serdar Durdagi
The Klotho is known as lifespan enhancing protein involved in antagonizing the effect of Wnt proteins. Wnt proteins are stem cell regulators, and uninterrupted exposure of Wnt proteins to the cell can cause stem and progenitor cell senescence, which may lead to aging. Keeping in mind the importance of Klotho in Wnt signaling, in silico approaches have been applied to study the important interactions between Klotho and Wnt3 and Wnt3a (wingless-type mouse mammary tumor virus (MMTV) integration site family members 3 and 3a)...
October 21, 2016: Journal of Enzyme Inhibition and Medicinal Chemistry
Christos Kontogiorgis, Maria Ntella, Lina Mpompou, Fotini Karallaki, Papadopoulos Athanasios, Dimitra Hadjipavlou-Litina, Diamanto Lazari
From the aerial parts of Thymus sibthorpii Bentham (Lamiaceae), five flavonoids apigenin (1), 7-methoxy-apigenin (2), naringenin (3), eriodictyol (4) and eriodictyol-7-glucoside (5), have been isolated together with caffeic acid methyl ester (6), rosmarinic acid (7) and rosmarinic acid methyl ester (8). The structures of the isolated compounds were established by spectroscopic methods. The extracts and the isolated compounds were tested for their free radical scavenging activity using the following in vitro assays: (i) interaction with the free stable radical of DPPH (1,1-diphenyl-2-picrylhydrazyl), (ii) inhibition of linoleic acid lipid peroxidation induced by the dihydrochloric acid of 2,2-azobis-2-amidinepropane (AAPH) and (iii) the scavenging activity of enzymatically produced superoxide anion...
September 9, 2016: Journal of Enzyme Inhibition and Medicinal Chemistry
Andrei Mocan, Gokhan Zengin, Gianina Crişan, Adriano Mollica
Considerable interest has been shown in natural sources and their compounds in developing new therapeutically agents for different diseases. In this framework, investigations performed on this topic play a central role for human health and drug development process. Schisandra chinensis (Turcz.) Baill is a medicinal and edible plant showing highly advantageous bioactivity and nutritional value. The main bioactive compounds from its fruits are lignans, derivatives of dibenzocyclooctadiene whereas concerning its leaves, phenolic acids, and flavonoids are dominant...
September 5, 2016: Journal of Enzyme Inhibition and Medicinal Chemistry
Cem Yamali, Halise Inci Gul, Hiroshi Sakagami, Claudiu T Supuran
Phenolic bis Mannich bases having the chemical structure of 1-[3,5-bis-aminomethyl-4-hydroxyphenyl]-3-(4-halogenophenyl)-2-propen-1-ones (1a-c, 2a-c, 3a-c) were synthesized (Numbers 1, 2, and 3 represent fluorine, chlorine, and bromine bearing compounds, respectively, while a, b, and c letters represent the compounds having piperidine, morpholine, and N-methyl piperazine) and their cytotoxic and carbonic anhydrase (CA, EC enzyme inhibitory effects were evaluated. Lead compounds should possess both marked cytotoxic potencies and selective toxicity for tumors...
September 4, 2016: Journal of Enzyme Inhibition and Medicinal Chemistry
Daniela De Vita, Fabiana Pandolfi, Luigi Ornano, Marta Feroci, Isabella Chiarotto, Ilaria Sileno, Federico Pepi, Roberta Costi, Roberto Di Santo, Luigi Scipione
A series of N,N-dimethylcarbamates containing a N,N-dibenzylamino moiety was synthesized and tested to evaluate their ability to inhibit Acetylcholinesterase (AChE). The most active compounds 4 and 8, showed 85 and 69% of inhibition at 50 μM, respectively. Furthermore, some basic SAR rules were outlined: an alkyl linker of six methylene units is the best spacer between the carbamoyl and dibenzylamino moieties; electron-withdrawal substituents on aromatics rings of the dibenzylamino group reduce the inhibitory power...
September 3, 2016: Journal of Enzyme Inhibition and Medicinal Chemistry
Anatolii R Syniugin, Olga V Ostrynska, Maksym O Chekanov, Galyna P Volynets, Sergiy A Starosyla, Volodymyr G Bdzhola, Sergiy M Yarmoluk
In this article, the derivatives of 3-quinoline carboxylic acid were studied as inhibitors of protein kinase CK2. Forty-three new compounds were synthesized. Among them 22 compounds inhibiting CK2 with IC50 in the range from 0.65 to 18.2 μM were identified. The most active inhibitors were found among tetrazolo-quinoline-4-carboxylic acid and 2-aminoquinoline-3-carboxylic acid derivatives.
September 2, 2016: Journal of Enzyme Inhibition and Medicinal Chemistry
Ashraf F Zaher, Suzan M Abuel-Maaty, Hala B El-Nassan, Samir A S Amer, Tamer M Abdelghany
Three series of benzothiophene derivatives were designed and synthesized as cytotoxic agents. The compounds were subjected to in vitro antitumor screening at the National Cancer Institute (NCI), Bethesda, MD. The results of the single dose screening indicated that only the benzothieno[3,2-b]pyran series 3a-f exhibited potent and broad spectrum cytotoxic activity and was subjected to five dose cytotoxic screening. The most active compound in this study was 2-amino-6-bromo-4-(4-nitrophenyl)-4H-[1]benzothieno[3,2-b]pyran-3-carbonitrile (3e) with MG-MID GI50, TGI, and LC50 values of 0...
September 2, 2016: Journal of Enzyme Inhibition and Medicinal Chemistry
Li Lang, Ningning Dong, Deyan Wu, Xue Yao, Weiqiang Lu, Chen Zhang, Ping Ouyang, Jin Zhu, Yun Tang, Wei Wang, Jian Li, Jin Huang
Human lipoxygenases (LOXs) have been emerging as effective therapeutic targets for inflammatory diseases. In this study, we found that four natural 2-arylbenzo[b]furan derivatives isolated from Artocarpus heterophyllus exhibited potent inhibitory activities against human LOXs, including moracin C (1), artoindonesianin B-1 (2), moracin D (3), moracin M (4). In our in vitro experiments, compound 1 was identified as the most potent LOX inhibitor and the moderate subtype selective inhibitor of 12-LOX. Compounds 1 and 2 act as competitive inhibitors of LOXs...
September 2, 2016: Journal of Enzyme Inhibition and Medicinal Chemistry
Kaan Kucukoglu, Fatih Oral, Tevfik Aydin, Cem Yamali, Oztekin Algul, Hiroshi Sakagami, Ilhami Gulcin, Claudiu T Supuran, Halise Inci Gul
A series of polymethoxylated-pyrazoline benzene sulfonamides were synthesized, investigated for their cytotoxic activities on tumor and non-tumor cell lines and inhibitory effects on carbonic anhydrase isoenzymes (hCA I and hCA II). Although tumor selectivity (TS) of the compounds were less than the reference compounds 5-Fluorouracil and Melphalan, trimethoxy derivatives 4, 5, and 6 were more selective than dimethoxy derivatives 2 and 3 as judged by the cytotoxicity assay with the cells both types originated from the gingival tissue...
August 31, 2016: Journal of Enzyme Inhibition and Medicinal Chemistry
Giannamaria Annunziato, Marco Pieroni, Roberto Benoni, Barbara Campanini, Thelma A Pertinhez, Chiara Pecchini, Agostino Bruno, Joana Magalhães, Stefano Bettati, Nina Franko, Andrea Mozzarelli, Gabriele Costantino
Cysteine is a building block for many biomolecules that are crucial for living organisms. O-Acetylserine sulfhydrylase (OASS), present in bacteria and plants but absent in mammals, catalyzes the last step of cysteine biosynthesis. This enzyme has been deeply investigated because, beside the biosynthesis of cysteine, it exerts a series of "moonlighting" activities in bacteria. We have previously reported a series of molecules capable of inhibiting Salmonella typhimurium (S. typhymurium) OASS isoforms at nanomolar concentrations, using a combination of computational and spectroscopic approaches...
August 31, 2016: Journal of Enzyme Inhibition and Medicinal Chemistry
Mahmoud A Al-Sha'er, Iman Mansi, Malak Khanfar, Alaa Abudayyh
The pharmacophoric features of the virtual cocrystallized protein of 178 Hsp90 proteins were obtained from the protein data bank and explored to generate 1260 pharmacophores evaluated using the decoy list composed of 1022 compounds. Accordingly, 51 pharmacophores were selected with high receiver operating characteristic (ROC) value for further processing. Subsequently, genetic algorithm and multiple linear regression analysis were employed to select an optimal combination of pharmacophoric models and 2D physicochemical descriptors capable of accessing a self-consistent quantitative structure-activity relationship (QSAR) of optimal predictive potential (R67(2) = 0...
August 28, 2016: Journal of Enzyme Inhibition and Medicinal Chemistry
Imdat Aygul, Fatma Yaylaci Karahalil, Claudiu T Supuran
Polyphenols are important secondary products of plants with the potential to inhibit carbonic anhydrases. The aim of this study was to investigate the inhibition effects of various phenolic standards, honey, propolis, and pollen species on human carbonic anhydrase I and II. The inhibition values (IC50) of the phenolics (gallic acid, protocatechuic acid, quercetin, catechin, tannic acid, and chrysin) ranged from 0.009 to 0.32 μg/mL, tannic acid emerging as the best inhibitor. The inhibition values of three different types of honey, heather, rhododendron, and chestnut ranged between 2...
August 25, 2016: Journal of Enzyme Inhibition and Medicinal Chemistry
Rana Abu Farha, Yasser Bustanji, Yusuf Al-Hiari, Tariq Al-Qirim, Ghassan Abu Shiekha, Rabab Albashiti
CONTEXT: Dyslipidemia is a major risk factor for the development of cardiovascular diseases. Many dyslipidemic patients do not achieve their target lipid levels with the currently available medications, and most of them may experience many side effects. OBJECTIVE: The present work aimed toward identifying a new class of novel nicotinic acid-carboxamide derivatives as promising antihyperlipidemic compounds. MATERIALS AND METHODS: Six novel N-(benzoylphenyl)pyridine-3-carboxamide derivatives were synthesized using acid chloride pathways...
August 25, 2016: Journal of Enzyme Inhibition and Medicinal Chemistry
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