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Sarah Allegra, Giovanna Fatiguso, Silvia De Francia, Fabio Favata, Elisa Pirro, Chiara Carcieri, Amedeo De Nicolò, Jessica Cusato, Giovanni Di Perri, Antonio D'Avolio
Mortality and morbidity due to invasive fungal infections have increased over the years. Posaconazole is a second-generation triazole agent with an extended spectrum of activity, which shows a high interindividual variability in its plasma levels, rendering dosing in many patients inconsistent or inadequate. Hence, posaconazole therapeutic drug monitoring, which is easily available in clinical practice, may improve treatment success and safety. The aim of the study was to describe posaconazole pharmacokinetics, and to evaluate the utility of therapeutic drug monitoring for therapy and prophylaxis in a cohort of adult patients...
November 20, 2017: Biomedicines
Eta Ashu, Ga Young Kim, Patrick Roy-Gayos, Kelly Dong, Adrian Forsythe, Victoria Giglio, Gregory Korfanty, Deborah Yamamura, Jianping Xu
Aspergillus fumigatus is a ubiquitous opportunistic fungal pathogen that can cause aspergillosis in humans. Over the last decade there have been increasing global reports of treatment failure due to triazole resistance. An emerging hypothesis states that agricultural triazole fungicide use causes clinical triazole-resistance. Here we test this hypothesis in Hamilton, Ontario, Canada by examining a total of 195 agricultural, urban and clinical isolates using 9 highly polymorphic microsatellite markers. For each isolate, the in vitro susceptibilities to itraconazole and voriconazole, two triazole drugs commonly used in the management of patients, were also determined...
November 20, 2017: Canadian Journal of Microbiology
Upendra Rao Anumala, Jo Waaler, Yves Nkizinkiko, Alexander Ignatev, Katina Lazarow, Peter Lindemann, Petter Angell Olsen, Sudarshan Murthy, Ezeogo Obaji, Alexander G Majouga, Sergey V Leonov, Jens Peter von Kries, Lari Lehtiö, Stefan Krauss, Marc Nazaré
A structure-guided hybridization approach using two privileged substructures gave instant access to a new series of tankyrase inhibitors. The identified inhibitor 16 displays high target affinity on tankyrase 1 and 2 with a biochemical and cellular IC50 values of 29 nM, 6.3 nM and 19 nM, respectively, and high selectivity towards other Poly(ADP-ribose) polymerase enzymes. The identified inhibitor shows a favorable in-vitro ADME profile as well as good oral bioavailability in mice, rats and dogs. Critical for the approach was the utilization of an appropriate linker between 1,2,4-triazole and benzimidazolone moieties, whereby a cyclobutyl linker displayed superior affinity compared to a cyclohexane and phenyl linker...
November 20, 2017: Journal of Medicinal Chemistry
Sujith Rajan, Surendra Puri, Durgesh Kumar, Madala Hari Babu, Kripa Shankar, Salil Varshney, Ankita Srivastava, Abhishek Gupta, M Sridhar Reddy, Anil N Gaikwad
Obesity and dyslipidemia is the two facet of metabolic syndrome, which needs further attention. Recent studies indicate triazole and indole derivatives have remarkable anti-obesity/antidyslipidemic activity. To harness the above-mentioned potential, a series of novel triazole clubbed indole derivatives were prepared using click chemistry and evaluated for anti-adipogenic activity. Based on the structure-activity relationship, essential functional groups which potentiate anti-adipogenic activity were identified...
October 16, 2017: European Journal of Medicinal Chemistry
M Wehbie, G Arrachart, L Ghannam, I Karamé, S Pellet-Rostaing
Solvent extraction of lanthanides Ln(iii) (La, Eu and Yb) with resorcin[4]arene cavitand-triazole-DODGA (CR4-TZ-DODGA) and t-butylcalix[4]arene-triazole-DODGA (C4-TZ-DODGA) has been studied in a room temperature ionic liquid (RTIL), N-octyl-N-ethylpiperidinium bis(trifluoromethylsulfonyl)imide ([EOPip]NTf2). The two macrocyclic platforms were functionalized with four diglycolamide (DGA) moieties thanks to a click reaction and fully characterized by NMR and MS analysis. The effects of acidity as well as the concentration of the ligands were investigated on the extraction and separation properties...
November 20, 2017: Dalton Transactions: An International Journal of Inorganic Chemistry
Chao-Jun Du, Xiao-Na Zhao, Bao-Yong Chen
In the title compound, [Co(C8H5O4)(C9H6N7)] n , the divalent Co(II) atom is six-coordinated to three N atoms from two symmetrical 5-(pyridin-4-yl)-1H,2'H-3,3'-bi[1,2,4-triazole] (H2pyttz) ligands and three O atoms from three symmetrical 3-carb-oxy-benzoate (Hbdic) ligands, leading to a distorted {CoN3O3} octa-hedral coordination environment. Two Co(II) cations are linked by four bridging carboxyl-ate groups to generate a dinuclear [Co2(CO2)4] unit. The dinuclear units are further connected into a chain along [010] via the Hbdic ligands...
November 1, 2017: Acta Crystallographica. Section E, Crystallographic Communications
Julio Zukerman-Schpector, Sofia Dallasta Pedroso, Lucas Sousa Madureira, Márcio Weber Paixão, Akbar Ali, Edward R T Tiekink
The mol-ecule in the title compound, C15H12N4O2, has a twisted L-shape with the dihedral angle between the aromatic rings of the N-bound benzene and C-bound benzyl groups being 70.60 (9)°. The nitro group is co-planar with the benzene ring to which it is connected [C-C-N-O torsion angle = 0.4 (3)°]. The three-dimensional packing is stabilized by a combination of methyl-ene-C-H⋯O(nitro), methyl-ene-C-H⋯π(phen-yl), phenyl-C-H⋯π(triazol-yl) and nitro-O⋯π(nitro-benzene) inter-actions, along with weak π(triazol-yl)-π(nitrobenzene) contacts [inter-centroid distance = 3...
November 1, 2017: Acta Crystallographica. Section E, Crystallographic Communications
Chao-Jun Du, Xiao-Na Zhao
In the title compound, [Co(C11H12NO6P)(C6H5N3)2]·C6H5N3, the 2,2'-[N-(phenyl-phospho-rylmethyl-κO)aza-nedi-yl]di-acetate dianion N,O,O',O''-chelates the Co(II) cation and two 1H-benzo[d][1,2,3]triazole mol-ecules coordinate to the Co(II) cation to complete the slightly distorted octa-hedral coordination. In the crystal, classical O-H⋯O, N-H⋯O hydrogen bonds and weak C-H⋯N hydrogen bonds link the mol-ecules into a three-dimensional supra-molecular architecture. π-π stacking between the triazole and benzene rings and between the benzene rings is also observed in the crystal...
November 1, 2017: Acta Crystallographica. Section E, Crystallographic Communications
Jennifer Weidhaas, Alexander Panaccione, Ananda Shankar Bhattacharjee, Ramesh Goel, Angela Anderson, Saraswati Poudel Acharya
Two sequencing batch reactors (SBRs) were run to bio-mineralize 2,4-dinitroanisole (DNAN) and 3-nitro-1,2,4-triazol-5-one (NTO) in lab scale settings. The reactors were shown to reproducibly biotransform these munitions under aerobic and anaerobic conditions during the operations of these SBRs. Complete removal (100% biotransformation) of DNAN (initially 17.7 ± 5.4 mg L(-1)) and NTO (initially 15.0 ± 7.1 mg L(-1)) was observed in an anaerobic SBR when Luria-Bertani (LB) broth was present. In contrast, an aerobic SBR degraded only 58 ± 22% of DNAN (initially 19...
November 16, 2017: Biodegradation
Angela P Van de Wouw, Vicki L Elliott, Steven Chang, Francisco J López-Ruiz, Steven J Marcroft, Alexander Idnurm
Leptosphaeria maculans is the major pathogen of canola (oilseed rape, Brassica napus) worldwide. In Australia, the use of azole fungicides has contributed to the 50-fold increase in canola production in the last 25 years. However, extensive application of fungicides sets the stage for the selection of fungal populations with resistance. A high-throughput in planta assay was developed to allow screening of thousands of isolates from multiple populations. Using this screen, isolates were identified with decreased sensitivity to the fungicide fluquinconazole when applied at field rates as a protective seed dressing: these isolates cause significantly larger lesions on cotyledons and true leaves and increased disease severity at plant maturity...
2017: PloS One
Michaela Bauer, Wei Wang, Mélanie L Lorion, Chuan Dong, Lutz Ackermann
Secondary C(sp3)-H arylations were accomplished by peptide bond isosteric triazoles in palladium catalysis. The unique power of this approach was reflected by enabling secondary C(sp3)-H functionalizations on terminal peptides as well as the unprecedented positional-selective C(sp3)-H functionalization of internal peptides, setting the stage for modular peptide late-stage diversification.
November 14, 2017: Angewandte Chemie
Krishnendu Maji, Debasish Haldar
We report a new synthetic aromatic ε-amino acid containing a triazole moiety with antimicrobial potential against Gram-positive, Gram-negative and pathogenic bacteria including Vibrio cholerae. Structure-property relationship studies revealed that all the functional groups are essential to enhance the antimicrobial activity. The 1-(2-aminophenyl)-1H-1,2,3-triazole-4-carboxylic acid was synthesized by click chemistry. From X-ray crystallography, the amino acid adopts a kink-like structure where the phenyl and triazole rings are perpendicular to each other and the amine and acid groups maintain an angle of 60°...
October 2017: Royal Society Open Science
Andrea Bistrović, Luka Krstulović, Anja Harej, Petra Grbčić, Mirela Sedić, Sanja Koštrun, Sandra Kraljević Pavelić, Miroslav Bajić, Silvana Raić-Malić
A series of novel amidino 2-substituted benzimidazoles linked to 1,4-disubstituted 1,2,3-triazoles were synthesized by implementation of microwave and ultrasound irradiation in click reaction and subsequent condensation of thus obtained 4-(1,2,3-triazol-1-yl)benzaldehyde with o-phenylenediamines. In vitro antiproliferative screening of compounds performed on human cancer cell lines revealed that p-chlorophenyl-substituted 1,2,3-triazolyl N-isopropylamidine 10c and benzyl-substituted 1,2,3-triazolyl imidazoline 11f benzimidazoles had selective and potent cytostatic activities in the low nM range against non-small cell lung cancer cell line A549, which could be attributed to induction of apoptosis and primary necrosis...
November 10, 2017: European Journal of Medicinal Chemistry
Junqi Wu, Tingjunhong Ni, Xiaoyun Chai, Ting Wang, Hongrui Wang, Jindong Chen, Yongsheng Jin, Dazhi Zhang, Shichong Yu, Yuanying Jiang
The incidence of life-threatening fungal infections has dramatically increased for decades. In order to develop novel antifungal agents, two series of (2R,3R)-1-(1H-1,2,4-triazol-1-yl)-2-(2,4-difluorophenyl)-3-(N-substitutied)-2-butanols (3a-o, 5a-f, 8a-u), which were analogues of voriconazole, were designed, synthesized and characterized by (1)H NMR, (13)C NMR and HRMS. The MIC80 values showed that the target compounds 3a-o indicated better activities than fluconazole on three important fungal pathogens except for 3i...
November 10, 2017: European Journal of Medicinal Chemistry
Bao-Lei Wang, Li-Yuan Zhang, Xing-Hai Liu, Yi Ma, Yan Zhang, Zheng-Ming Li, Xiao Zhang
A series of new 3-substitutedphenyl-4-substitutedbenzylideneamino-1,2,4-triazole Mannich bases and bis-Mannich bases were synthesized through Mannich reaction with high yields. Their structures were confirmed by means of IR, (1)H NMR, (13)C NMR and elemental analysis. The preliminary bioassay indicated that compounds 7g, 7h and 7l exhibited potent in vitro inhibitory activities against ketol-acid reductoisomerase (KARI) with Ki value of (0.38 ± 0.25), (6.59 ± 2.75) and (8.46 ± 3.99) μmol/L, respectively, and were comparable with IpOHA...
November 10, 2017: Bioorganic & Medicinal Chemistry Letters
Mahalakshmi Thillainayagam, Kullappan Malathi, Sudha Ramaiah
The structural motifs of chalcones, flavones and triazoles with varied substitutions have been studied for the anti-malarial activity. In this study, 25 novel derivatives of chalcone and flavone hybrid derivatives with 1, 2, 3 - triazole linkage are docked with Plasmodium falciparum dihydroorotate dehydrogenase to establish their inhibitory activity against Plasmodium falciparum. The best binding conformation of the ligands at the catalytic site of dihydroorotate dehydrogenase are selected to characterize the best bound ligand using the best consensus score and the number of hydrogen bond interactions...
November 13, 2017: Journal of Biomolecular Structure & Dynamics
Chin M Wong, Matthew B Peterson, Indrek Pernik, Roy T McBurney, Barbara A Messerle
Rhodium(I) complexes were explored as catalysts for the hydrogen borrowing reactions of amines and alcohols. Bidentate carbene-triazole ligands were readily synthesized via "click" reactions which allowed a diversity of ligand backbones to be accessed. The catalytic transformations are highly efficient, able to reach completion in under 6 h, and promote C-N bond formation across a range of primary alcohol and amine substrates. Moreover, site-selective catalysis can be achieved using substrates with more than one reactive site...
November 13, 2017: Inorganic Chemistry
Ashleigh S Paparella, Kwang Jun Lee, Andrew J Hayes, Jiage Feng, Zikai Feng, Danielle Cini, Sonali Deshmukh, Grant W Booker, Matthew C J Wilce, Steven W Polyak, Andrew D Abell
We report the synthesis and evaluation of 5-halogenated-1,2,3-triazoles as inhibitors of biotin protein ligase from Staphylococcus aureus. The halogenated compounds exhibit significantly improved antibacterial activity over their nonhalogenated counterparts. Importantly, the 5-fluoro-1,2,3-triazole compound 4c displays antibacterial activity against S. aureus ATCC49775 with a minimum inhibitory concentration (MIC) of 8 μg/mL.
November 16, 2017: ACS Infectious Diseases
Nilufer Bulut, Umit M Kocyigit, Ibrahim H Gecibesler, Taner Dastan, Huseyin Karci, Parham Taslimi, Sevgi Durna Dastan, Ilhami Gulcin, Ahmet Cetin
Some novel derivatives of thiosemicarbazide and 1,2,4-triazole-3-thiol were synthesized and evaluated for their biological activities. The title compounds were prepared starting from readily available pyridine-2,5-dicarboxylic acid. The reaction carboxylic acid with absolute ethanol afforded the corresponding dimethyl pyridine-2,5-dicarboxylate (1). The reaction of dimethyl-2,5-pyridinedicarboxylate (1) with hydrazine hydrate good yielded pyridine-2,5-dicarbohydrazide (2). Refluxing compound 2 with alkyl/aryl isothiocyanate derivatives for 3-8 h afforded 1,4-disubstituted thiosemicarbazides (3a-e)...
November 13, 2017: Journal of Biochemical and Molecular Toxicology
Chandra M R Volla, Kuntal Pal, Abdul Hoque
A convenient and simple, Rh(II)-catalyzed denitrogenative methodology for the synthesis of biologically interesting 2-amino-benzoxazinones and 5-amino-oxadiazoles from readily available isatoic anhydrides and oxadiazolones has been developed. These reactions proceed via an O-H insertion onto α-imino Rh(II)-carbenoid species followed by a rearrangement. The scope of the reaction can also be extended to benzoxazinones to access amino-substituted benzoxazines.
November 13, 2017: Chemistry: a European Journal
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