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Sajjad H Sumrra, Fazila Mushtaq, Muhammad Khalid, Muhammad Asam Raza, Muhammad Faizan Nazar, Bakhat Ali, Ataualpa A C Braga
Biologically active triazole Schiff base ligand (L) and metal complexes [Fe(II), Co(II), Ni(II), Cu(II) and Zn(II)] are reported herein. The ligand acted as tridentate and coordinated towards metallic ions via azomethine-N, triazolic-N moiety and deprotonated-O of phenyl substituents in an octahedral manner. These compounds were characterized by physical, spectral and analytical analysis. The synthesized ligand and metal complexes were screened for antibacterial pathogens against Chromohalobacter salexigens, Chromohalobacter israelensi, Halomonas halofila and Halomonas salina, antifungal bioassay against Aspergillus niger and Aspergellus flavin, antioxidant (DPPH, phosphomolybdate) and also for enzyme inhibition [butyrylcholinesterase (BChE) and acetylcholinesterase (AChE)] studies...
September 13, 2017: Spectrochimica Acta. Part A, Molecular and Biomolecular Spectroscopy
Naila A Mugheirbi, Peter O'Connell, Dolores R Serrano, Anne Marie Healy, Lynne S Taylor, Lidia Tajber
Fluid bed coating offers potential advantages as a formulation platform for amorphous solid dispersions (ASDs) of poorly soluble drugs, being a one-step manufacturing process which could reduce the risk of phase separation associated with multiple step manufacturing approaches. However, the impact of the physicochemical nature of carrier spheres on the properties and drug release from the ASDs has not been studied in detail. In this work, tartaric acid (TAP) and microcrystalline cellulose (CEL) spheres were chosen as examples of functional and inert beads, respectively...
September 18, 2017: Molecular Pharmaceutics
Sanjit Das, Khoubaib Ben Haj Salah, Emmanuel Wenger, Jean Martinez, Jules Kotarba, Vanessa Andreu, Nicolas Ruiz, Filippo Savini, Lorenzo Stella, Claude Didierjean, Baptiste Legrand, Nicolas Inguimbert
We propose a simple and efficient strategy to significantly improve the antibacterial activity of peptaibols and other antimicrobial peptides by N-terminal capping with 1,2,3-triazole bearing various hydrophobic substituents on C-4. We showed, herein, that such N-terminal insertions on alamethicin F50/5 could enhance its antimicrobial activity on gram-positive bacteria without modification of its overall three-dimensional structure. Indeed, while the native peptide and its analogues shared comparable helical contents, the crystal structure of one of the most active derivative showed a local slight distortion of the N-terminal extremity, which was also observed in solution using NMR spectroscopy...
September 18, 2017: Chemistry: a European Journal
Xin Li, Qi Yang, Qing Wei, Gang Xie, Sanping Chen, Shengli Gao
The design and synthesis of explosives with high performance, good thermal stability, and low sensitivity is an important subject for the development of energetic materials. Energetic complexes have recently emerged as a promising energetic material form. As one of the representatives, [Cu(Htztr)2(H2O)2]n (H2tztr = 3-(1H-tetrazol-5-yl)-1H-triazole) was previously reported with good energetic performance, outstanding thermostability (Tdec = 345 °C) and low sensitivity to impact and friction stimuli. However, due to the existence of water molecules, its effective energy density is remarkably decreased, resulting in a diminished detonation performance...
September 18, 2017: Dalton Transactions: An International Journal of Inorganic Chemistry
Dana M Lindemann, Matthew C Allender, Marta Rzadkowska, Grace Archer, Lauren Kane, Eric Baitchman, Elizabeth A Driskell, Caroline T Chu, Kuldeep Singh, Shih-Hsuan Hsiao, John M Sykes, Sherry Cox
Snake fungal disease (SFD; Ophidiomyces ophiodiicola) is posing a significant threat to several free-ranging populations of pitvipers. Triazole antifungals have been proposed for the treatment of mycoses in reptiles; however, data are lacking about their safety and efficacy in snakes with SFD. Study 1 investigated in vitro susceptibility, and identified that plasma concentrations >250 ng/ml (voriconazole) and >1,000 ng/ml (itraconazole) may be effective in vivo for SFD. In Study 2, the pharmacokinetics after a single subcutaneous voriconazole injection were assessed in apparently healthy free-ranging cottonmouths (Agkistrodon piscivorus)...
September 2017: Journal of Zoo and Wildlife Medicine: Official Publication of the American Association of Zoo Veterinarians
Grégorio Crini, Adeline Exposito Saintemarie, Steffi Rocchi, Marc Fourmentin, Audrey Jeanvoine, Laurence Millon, Nadia Morin-Crini
In this study, an adsorption-oriented process for the removal of fungicides from polycontaminated aqueous solutions was applied. To remove triazole fungicides from aqueous mixtures of propiconazole (PROPI), tebuconazole (TEBU), epoxiconazole (EPOXI), bromuconazole (BROMU) and difenoconazole (DIFENO), several materials used as adsorbents were compared using batch experiments, namely two conventional activated carbons (ACs) and five nonconventional cross-linked cyclodextrin (CD)-based materials (α-CDP, β-CDP, γ-CDP, αβγ-CDP mixture, and hydroxypropyl-β-CDP)...
August 2017: Heliyon
Fengnian Zhao, Yongxin She, Chao Zhang, Xiaolin Cao, Shanshan Wang, Lufei Zheng, Maojun Jin, Hua Shao, Fen Jin, Jing Wang
A selective analytical method for the simultaneous determination of 20 triazole fungicides and plant growth regulators in cucumber samples was developed using solid-phase extraction with specific molecularly imprinted polymers (MIPs) as adsorbents. The MIPs were successfully prepared by precipitation polymerization using triadimefon as the template molecule, methacrylic acid as the functional monomer, trimethylolpropane trimethacrylate as the crosslinker, and acetonitrile as the porogen. The performance and recognition mechanism for both the MIPs and non-molecularly imprinted polymers were evaluated using adsorption isotherms and adsorption kinetics...
August 22, 2017: Journal of Chromatography. B, Analytical Technologies in the Biomedical and Life Sciences
Hiroyuki Kobayashi, Takashi Misawa, Kenji Matsuno, Yosuke Demizu
Preorganized cyclic α,α-disubstituted α-amino acids (dAA) bearing functionalized side chains that acted as peptide-helix inducers, which could be used for solid-phase peptide synthesis, were designed and synthesized. Furthermore, a helical octapeptide with the following amino acid sequence was prepared, and its preferred conformation was analyzed based on its CD spectra: Ac-X(1)EYSAX(2)KA-NH2 (11: X(1) = Api(C4N3), X(2) = Ac6c). The side-chain azido functional group of peptide 11 was efficiently converted to various 1,2,3-triazole groups via Huisgen 1,3-dipolar cycloaddition reactions involving different types of alkynes...
September 15, 2017: Journal of Organic Chemistry
Zipeng Gong, Yaping Peng, Jie Qiu, Anbai Cao, Guangcheng Wang, Zhiyun Peng
Benzothiazole-triazole derivatives 6a-6s have been synthesized and characterized by ¹HNMR and (13)C-NMR. All synthetic compounds were screened for their in vitro α-glucosidase inhibitory activity by using Baker's yeast α-glucosidase enzyme. The majority of compounds exhibited a varying degree of α-glucosidase inhibitory activity with IC50 values between 20.7 and 61.1 μM when compared with standard acarbose (IC50 = 817.38 μM). Among the series, compound 6s (IC50 = 20.7 μM) bearing a chlorine group at the 5-position of the benzothiazole ring and a tertbutyl group at the para position of the phenyl ring, was found to be the most active compound...
September 15, 2017: Molecules: a Journal of Synthetic Chemistry and Natural Product Chemistry
Russell E Lewis, Paul E Verweij
Infections caused by triazole-resistant Aspergillus fumigatus are associated with a higher probability of treatment failure and mortality. Because clinical experience in managing these infections is still limited, mouse models of invasive aspergillosis fulfill a critical void for studying treatment regimens designed to overcome resistance. The type of immunosuppression, the route of infection, the timing of antifungal administration, and the end points used to assess antifungal activity affect the interpretation of data from these models...
August 15, 2017: Journal of Infectious Diseases
Anuradha Chowdhary, Cheshta Sharma, Jacques F Meis
Aspergillus fumigatus remains the most common species in all pulmonary syndromes, followed by Aspergillus flavus which is a common cause of allergic rhinosinusitis, postoperative aspergillosis and fungal keratitis. The manifestations of Aspergillus infections include invasive aspergillosis, chronic pulmonary aspergillosis and bronchitis. Allergic manifestations of inhaled Aspergillus include allergic bronchopulmonary aspergillosis and severe asthma with fungal sensitization. Triazoles are the mainstay of therapy against Aspergillus infections for treatment and prophylaxis...
August 15, 2017: Journal of Infectious Diseases
Lucia Riera, Julio Pérez, Sergio Fombona, Jesús Díaz
Unsupported 1-methyl-1,2,3-triazole has been coordinated to {Mo(3-methallyl)(CO)2(N-N)} (N-N= 2,2'-bipyridine, bipy; or 1,10-phenanthroline,phen) fragments yielding cationic complexes which can be regarded as metalated triazolium salts. Their reactivity towards a strong base led to the deprotonation of the C5-H group of the triazole moiety, followed by an intermolecular nucleophilic attack to the ortho CH group of a bipy or phen ligand affording cyclic, bimetallic dearomatized C-C coupling products. The reaction of the neutral bipy derivative with an acid led to the formation of dihydropyridyl units by protonation of a CH group of the dearomatized rings, the dimeric nature of complexes being mantained upon protonation...
September 14, 2017: Chemistry: a European Journal
Urša Pečar Fonović, Ana Mitrović, Damijan Knez, Tanja Jakoš, Anja Pišlar, Boris Brus, Bojan Doljak, Jure Stojan, Simon Žakelj, Jurij Trontelj, Stanislav Gobec, Janko Kos
Cathepsin X is a cysteine peptidase involved in the progression of cancer and neurodegenerative diseases. Targeting this enzyme with selective inhibitors opens a new possibility for intervention in several therapeutic areas. In this study triazole-based reversible and selective inhibitors of cathepsin X have been identified. Their selectivity and binding is enhanced when the 2,3-dihydrobenzo[b][1,4]dioxine moiety is present as the R(1) substituent. Of a series of selected triazole-benzodioxine derivatives, compound 22 is the most potent inhibitor of cathepsin X carboxypeptidase activity (Ki = 2...
September 13, 2017: Scientific Reports
Serena Massari, Jenny Desantis, Giulio Nannetti, Stefano Sabatini, Sara Tortorella, Laura Goracci, Violetta Cecchetti, Arianna Loregian, Oriana Tabarrini
Two facile and efficient one-step procedures for the regioselective synthesis of 7-aryl-5-methyl- and 5-aryl-7-methyl-2-amino-[1,2,4]triazolo[1,5-a]pyrimidines have been developed, via reactions of 3,5-diamino-1,2,4-triazole with variously substituted 1-aryl-1,3-butanediones and 1-aryl-2-buten-1-ones, respectively. The excellent yield and/or regioselectivity shown by the reactions decreased when ethyl 5-amino-1,2,4-triazole-3-carboxylate was used. [1,2,4]Triazolo[1,5-a]pyrimidine being a privileged scaffold, the procedures herein reported may be useful for the preparation of biologically active compounds...
September 13, 2017: Organic & Biomolecular Chemistry
Myungsun Shin, Helena W Snyder, Giulia Donvito, Lesley D Schurman, Todd E Fox, Aron H Lichtman, Mark Kester, Ku-Lung Hsu
Diacylglycerol lipase-beta (DAGLβ) hydrolyzes arachidonic acid (AA)-containing diacylglycerols to produce bioactive lipids including endocannabinoids and AA-derived eicosanoids involved in regulation of inflammatory signaling. Previously, we demonstrated that DAGLβ inactivation using the triazole urea inhibitor KT109 blocked macrophage inflammatory signaling and reversed allodynic responses of mice in inflammatory and neuropathic pain models. Here, we tested whether we could exploit the phagocytic capacity of macrophages to localize delivery of DAGLβ inhibitors to these cells in vivo using liposome encapsulated KT109...
September 13, 2017: Molecular Pharmaceutics
Michal Jakl, Jindřich Fanfrlík, Jana Jaklová Dytrtová
RATIONALE: Frequently used pesticide cyproconazole (Cyp) interacts with essential elements commonly present in soil and playing important roles in various enzymatic processes. These interactions predetermine Cyp degradation pathways. We suggest a simple experimental and theoretical approach for the prediction of pesticides behavior. METHODS: Cu/Cyp complexes are explored because of the typical Cu(II) reduction in complexes. Its level and the stability of Cu-ligand bond depend on the type and the number of the surrounding ligands...
September 12, 2017: Rapid Communications in Mass Spectrometry: RCM
Clara E Negri, Sarah S Gonçalves, Ana Cristina P Sousa, Maria Daniela Bergamasco, Marinês D V Martino, Flavio Queiroz-Telles, Valerio Rodrigues Aquino, Paulo de Tarso O Castro, Ferry Hagen, Jacques F Meis, Arnaldo L Colombo
Aspergillus fumigatus azole resistance has globally emerged as a health problem. We evaluated the in vitro antifungal susceptibility of 221 clinical A. fumigatus isolates according to CLSI. Sixty-one isolates exhibiting MIC at the epidemiological cut-off value (ECV) for itraconazole or above ECV for any triazole were checked for CYP51A mutations. No mutations were documented, even for four isolates (1.8%) with high voriconazole MICs, indicating that triazoles may be safely used to treat aspergillosis in Brazil...
September 11, 2017: Antimicrobial Agents and Chemotherapy
Marc Lamshoeft, Zhenglei Gao, Herbert Resseler, Carola Schriever, Robin Sur, Paul Sweeney, Sarah Webb, Birgit Zillgens, Marco U Reitz
A new hydroponic study design to determine uptake of chemicals by plant roots was tested by (i) investigating uptake of [(14)C]-1,2,4-triazole by wheat plants in a ring test with ten laboratory organizations and (ii) studying uptake of ten other radiolabelled chemicals by potato, tomato or wheat plants in two laboratories. Replicate data from the ring test were used to calculate plant uptake factor (PUF) values (uptake into roots and shoots) and transpiration stream concentration factor (TSCF) values (uptake into shoots)...
September 8, 2017: Science of the Total Environment
Ling Yang, Ying Wang, Yanke Che, Hua Jiang
A novel aryl-triazole foldamer incorporating a 1,8-naphthalimide motif was designed and synthesized. (1)H NMR, UV-vis and fluorescence spectroscopic titration experiments with halide anions (Cl(-), Br(-), I(-)) demonstrated that the π-π stacking interaction of 1,8-naphthalimide building blocks could largely enhance the folding and anion binding of the foldamer.
September 11, 2017: Organic & Biomolecular Chemistry
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 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
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