Journal of Enzyme Inhibition and Medicinal Chemistry, Volume 31, Issue 2 (2016)

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Journal of Enzyme Inhibition and Medicinal Chemistry, Volume 31, Issue 2 (2016)

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Review Article

Recent advances in novel heterocyclic scaffolds for the treatment of drug-resistant malaria
Sahil Kumar, Rajesh K. Singh, Babita Patial, Sachin Goyal & T. R. Bhardwaj
Pages: 173-186
Published online: 16 Mar 2015
AbstractforRecent advances in novel heterocyclic scaffolds for the treatment of drug-resistant malaria | Full Text | References | PDF (2.4 MB)
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Unifi nootropics from the lab to the web: a story of academic (and industrial) shortcomings
Fulvio Gualtieri
Pages: 187-194
Published online: 01 Apr 2015
AbstractforUnifi nootropics from the lab to the web: a story of academic (and industrial) shortcomings | Full Text | References | PDF (466.5 KB) | Supplemental
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Research Article

Article
Pyrazolo[1,5-a]quinazoline scaffold as 5-deaza analogue of pyrazolo[5,1-c][1,2,4]benzotriazine system: synthesis of new derivatives, biological activity on GABAA receptor subtype and molecular dynamic study
Gabriella Guerrini, Giovanna Ciciani, Samuele Ciattini, Letizia Crocetti, Simona Daniele, Claudia Martini, Fabrizio Melani, Claudia Vergelli & Maria Paola Giovannoni
Pages: 195-204
Published online: 20 Mar 2015
AbstractforPyrazolo[1,5-a]quinazoline scaffold as 5-deaza analogue of pyrazolo[5,1-c][1,2,4]benzotriazine system: synthesis of new derivatives, biological activity on GABAA receptor subtype and molecular dynamic study | Full Text | References | PDF (1.3 MB) | Supplemental
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Article
Synthesis and inhibition potency of novel ureido benzenesulfonamides incorporating GABA as tumor-associated carbonic anhydrase IX and XII inhibitors
Mariangela Ceruso, Sabrina Antel, Andrea Scozzafava & Claudiu T. Supuran
Pages: 205-211
Published online: 20 Mar 2015
AbstractforSynthesis and inhibition potency of novel ureido benzenesulfonamides incorporating GABA as tumor-associated carbonic anhydrase IX and XII inhibitors | Full Text | References | PDF (410.5 KB) | Supplemental
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Article
Crocus cancellatus subsp. damascenus stigmas: chemical profile, and inhibition of α-amylase, α-glucosidase and lipase, key enzymes related to type 2 diabetes and obesity
Monica R. Loizzo, Mariangela Marrelli, Alessandro Pugliese, Filomena Conforti, Farsad Nadjafi, Francesco Menichini & Rosa Tundis
Pages: 212-218
Published online: 20 Mar 2015
AbstractforCrocus cancellatus subsp. damascenus stigmas: chemical profile, and inhibition of α-amylase, α-glucosidase and lipase, key enzymes related to type 2 diabetes and obesity | Full Text | References | PDF (369.7 KB)
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Article
Synthesis and biological evaluation of novel 3-substituted amino-4-hydroxylcoumarin derivatives as chitin synthase inhibitors and antifungal agents
Zhiqiang Ge, Qinggang Ji, Chunyan Chen, Qin Liao, Hualong Wu, Xiaofei Liu, Yanrong Huang, Lvjiang Yuan & Fei Liao
Pages: 219-228
Published online: 27 Mar 2015
AbstractforSynthesis and biological evaluation of novel 3-substituted amino-4-hydroxylcoumarin derivatives as chitin synthase inhibitors and antifungal agents | Full Text | References | PDF (333.4 KB) | Supplemental
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Article
Evaluation of N-acetyl-S-(p-chlorophenylcarbamoyl)cysteine as an irreversible inhibitor of mammalian thioredoxin reductase1
Wei Chen, Zhiming Jiang, Nengming Lin, Zhiguo Zheng, Zhongjian Chen, Xiaoying Zhang & Xiangming Guan
Pages: 229-235
Published online: 17 Mar 2015
AbstractforEvaluation of N-acetyl-S-(p-chlorophenylcarbamoyl)cysteine as an irreversible inhibitor of mammalian thioredoxin reductase1 | Full Text | References | PDF (469.5 KB)
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Article
Design, synthesis, antimicrobial evaluation and molecular docking studies of some new 2,3-dihydrothiazoles and 4-thiazolidinones containing sulfisoxazole
Tamer Nasr, Samir Bondock & Sameh Eid
Pages: 236-246
Published online: 27 Mar 2015
AbstractforDesign, synthesis, antimicrobial evaluation and molecular docking studies of some new 2,3-dihydrothiazoles and 4-thiazolidinones containing sulfisoxazole | Full Text | References | PDF (904.4 KB) | Supplemental
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Article
An alternative purification method for human serum paraoxonase 1 and its interactions with anabolic compounds
Dudu Demir, Nahit Gencer & Oktay Arslan
Pages: 247-252
Published online: 20 Mar 2015
AbstractforAn alternative purification method for human serum paraoxonase 1 and its interactions with anabolic compounds | Full Text | References | PDF (278.2 KB)
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Article
2-Alkyl(aryl)-quinazolin-4(3H)-thiones, 2-R-(quinazolin-4(3H)-ylthio)carboxylic acids and amides: synthesis, molecular docking, antimicrobial and anticancer properties
Lyudmyla Antypenko, Sergiy Kovalenko, Yulia Posylkina, Vladyslav Nikitin, Natalia Fedyunina & Vitalii Ivchuk
Pages: 253-265
Published online: 01 Apr 2015
Abstractfor2-Alkyl(aryl)-quinazolin-4(3H)-thiones, 2-R-(quinazolin-4(3H)-ylthio)carboxylic acids and amides: synthesis, molecular docking, antimicrobial and anticancer properties | Full Text | References | PDF (1 MB) | Supplemental
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Article
Antioxidant, antiradical, and anticholinergic properties of cynarin purified from the Illyrian thistle (Onopordum illyricum L.)
Meryem Topal, Hulya Gocer, Fevzi Topal, Pınar Kalin, Leyla Polat Köse, İlhami Gülçin, Kader C. Çakmak, Murat Küçük, Lokman Durmaz, Ahmet C. Gören & Saleh H. Alwasel
Pages: 266-275
Published online: 20 Mar 2015
AbstractforAntioxidant, antiradical, and anticholinergic properties of cynarin purified from the Illyrian thistle (Onopordum illyricum L.) | Full Text | References | PDF (587.9 KB)
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Article
The slow dissociation rate of K-1602 contributes to the enhanced inhibitory activity of this novel alkyl–aryl-bearing fluoroketolide
Marios Krokidis, Anthony Bougas, Maria Stavropoulou, Dimitrios Kalpaxis & George P. Dinos
Pages: 276-282
Published online: 25 Mar 2015
AbstractforThe slow dissociation rate of K-1602 contributes to the enhanced inhibitory activity of this novel alkyl–aryl-bearing fluoroketolide | Full Text | References | PDF (432 KB)
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Article
Convergent QSAR studies on a series of NK3 receptor antagonists for schizophrenia treatment
Marina Candido Primi, Vinícius Gonçalves Maltarollo, Juliana Gallottini Magalhães, Matheus Malta de Sá, Carlota Oliveira Rangel-Yagui & Gustavo Henrique Goulart Trossini
Pages: 283-294
Published online: 09 Apr 2015
AbstractforConvergent QSAR studies on a series of NK3 receptor antagonists for schizophrenia treatment | Full Text | References | PDF (3.1 MB) | Supplemental
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Article
Bicyclic γ-amino acids as inhibitors of γ-aminobutyrate aminotransferase
Andrea Pinto, Lucia Tamborini, Eugenia Pennacchietti, Antonio Coluccia, Romano Silvestri, Gregorio Cullia, Carlo De Micheli, Paola Conti & Daniela De Biase
Pages: 295-301
Published online: 25 Mar 2015
AbstractforBicyclic γ-amino acids as inhibitors of γ-aminobutyrate aminotransferase | Full Text | References | PDF (556.6 KB) | Supplemental
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Article
Simple chalcones and bis-chalcones ethers as possible pleiotropic agents
Thalia Liargkova, Dimitra J. Hadjipavlou-Litina, Caterina Koukoulitsa, Efstathia Voulgari & Constantinos Avgoustakis
Pages: 302-313
Published online: 23 Mar 2015
AbstractforSimple chalcones and bis-chalcones ethers as possible pleiotropic agents | Full Text | References | PDF (1.3 MB)
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Article
In vitro effects of some flavonoids and phenolic acids on human pyruvate kinase isoenzyme M2
Erdem Aslan, Caglar Guler & Sevki Adem
Pages: 314-317
Published online: 23 Mar 2015
AbstractforIn vitro effects of some flavonoids and phenolic acids on human pyruvate kinase isoenzyme M2 | Full Text | References | PDF (372.6 KB)
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Article
3-Methyl-2-phenyl-1-substituted-indole derivatives as indomethacin analogs: design, synthesis and biological evaluation as potential anti-inflammatory and analgesic agents
Khaled R. A. Abdellatif, Phoebe F. Lamie & Hany A. Omar
Pages: 318-324
Published online: 23 Mar 2015
Abstractfor3-Methyl-2-phenyl-1-substituted-indole derivatives as indomethacin analogs: design, synthesis and biological evaluation as potential anti-inflammatory and analgesic agents | Full Text | References | PDF (528 KB)
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Article
Partial purification and characterization of lipase from Geobacillus stearothermophilus AH22
Arife Pınar Ekinci, Barbaros Dinçer, Nimet Baltaş & Ahmet Adıgüzel
Pages: 325-331
Published online: 23 Mar 2015
AbstractforPartial purification and characterization of lipase from Geobacillus stearothermophilus AH22 | Full Text | References | PDF (700.8 KB)
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Short Communication

Rapid Communication
Peptidomimetic ethyl propenoate covalent inhibitors of the enterovirus 71 3C protease: a P2–P4 study
Melgious J. Y. Ang, Qiu Ying Lau, Fui Mee Ng, Siew Wen Then, Anders Poulsen, Yuen Kuen Cheong, Zi Xian Ngoh, Yong Wah Tan, Jianhe Peng, Thomas H. Keller, Jeffrey Hill, Justin J. H. Chu & C. S. Brian Chia
Pages: 332-339
Published online: 20 Mar 2015
AbstractforPeptidomimetic ethyl propenoate covalent inhibitors of the enterovirus 71 3C protease: a P2–P4 study | Full Text | References | PDF (1.5 MB) | Supplemental
  • 1410 Views
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Rapid Communication
Abl1 inhibitory contaminants leach from plastic tubes
Hui Chen, Bart Blanchaert, Abhijit Babaji Shinde, Erwin Adams, Jef Rozenski, Myriam Baes & Ann Van Schepdael
Pages: 340-343
Published online: 23 Mar 2015
AbstractforAbl1 inhibitory contaminants leach from plastic tubes | Full Text | References | PDF (588 KB)
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