This paper describes the antiviral evaluation of new N-amino-1,2,3-triazole derivatives, 1-(substituted-phenylamino)-5-methyl-1H-[1,2,3]-triazole-4-carboxylic acid ethyl esters, 3 and 1-(4-substituted-phenylamino)-5-methyl-1H-[1,2,3]-triazole-4-carboxylic acid hydrazides, 4, on Cantagalo virus r...
A novel structural class of glycogen synthase kinase-3β inhibitors is modeled using quantum mechanics, automated docking, and molecular dynamics simulations. The proposed binding modes identify important hydrogen bonds and salt-bridges with the ATP-binding pocket of the kinase. The modeled comp...
A novel series of conjugates of benzosuberone and 1,2,3-triazole i.e. 3-(4-phenyl-1H-1,2,3-triazol-1-yl)propyl-9-chloro-2,3-dimethyl-6,7-dihydro-5H-benzo[7]annulene-8-carboxylic acids (8a-j) were synthesized in good to excellent yields catalysed by CuSO4 under milder reaction conditions and eval...
Candida is an important opportunistic human fungal pathogen. The cis-2-dodecenoic acid (BDSF) showing in vitro activity of against C. albicans growth, germ-tube germination and biofilm formation has been a potential inhibitor for Candida and other fungi. In this study, facile synthetic strategie...
Efficient Pd(0)-catalysed synthesis of 5-alkynyl-1-β-d-ribofuranosyl-1H-[1,2,3]triazole-4-carboxylic acid amide depends on the presence of different protecting groups of the ribose moiety. Peracetylated 5-iodo substrate (15) couples with terminal alkynes or trimethyl-[(tributylstannyl)ethynyl]s...
5-Methyl-2-phenyl-2H-1,2,3-triazole-4-carboxylic acid (MPTC), a newly synthesized compound, was explored to study the structural properties and theoretical spectra by using GaussView5.0 program package and the time dependent density functional theory (TD DFT). The calculated quantum chemical val...
A novel series of biscoumarin-1,2,3-triazole hybrids 6a-n was prepared and evaluated for α-glucosidase inhibitory potential. All fourteen derivatives exhibited excellent α-glucosidase inhibitory activity with IC50 values ranging between 13.0 ± 1.5 and 75.5 ± 7.0 µM when compared with the ac...
Inhibiting the decomposition of carbohydrates into glucose or promoting glucose conversion is considered to be an effective treatment for type 2 diabetes. Herein, a series of novel xanthone-triazole derivatives were designed, synthesized, and their α-glucosidase inhibitory activities and glucos...
A series of 1-substituted benzyl-4-[1-phenyl-3-(4-methyl-2-aryl-1,3-thiazol-5-yl)-1H-pyrazol-4-yl]-1H-1,2,3-triazole derivatives (7a-y) have been synthesized by click reaction of 5-(4-ethynyl-1-phenyl-1H-pyrazol-3-yl)-4-methyl-2-aryl-1,3-thiazole (5a-e) with substituted benzyl azide. The startin...
1,4-Disubstituted-1,2,3-triazoles (3–27) have been synthesized by [3+2] cycloaddition of different 2-(azidomethyl)-dihydronaptho(benzo)furans (2a, 2b, 2c and 2d) with different alkynes. All the compounds were screened for antitubercular activity against Mycobacterium tuberculosis H37Rv. Compoun...
The methyl 1-benzyl-1H-1,2,3-triazole-4-carboxylate (C11H11N3O2) has been studied by theoretically methods. The structure of this compound is optimized by density functional theory (DFT), the second-order Møller–Plesset perturbation theory (MP2) and G3 theory (G3(MP2)) levels. Our calculation r...
To avoid production of a phospholipidosis-inducing metabolite, we replaced the amide structure of SUN13837 (1) with a 1,2,3-triazole. The resulting 1,2,3-triazole analog of 1 (compound 2) displayed greater neuroprotective activity than 1. Structural modification of 2 yielded compound 10, which s...
The reaction of the ligand [1-(4-((1H-benzo[d][1,2,3]triazol-2(3H)-yl)methyl)benzyl)-1H-benzo[d][1,2,3]triazole] (L) with CuCl2 in acetonitrile yields a dinuclear copper(II) complex [Cu2Cl4L2]·2CH3CN (1·2CH3CN), which has been characterized by elemental analysis, powder and single crystal X-ra...
An efficient route, not including any metal salt as a catalyst, for the synthesis of a new 2-substituted 1,2,3- triazole-1-oxide is reported in this paper. The title compound has been synthesized via reacting 4-(methyl)isonitrosoacetophenone with hydrazine hydrate and dipyridyl ketone in high yi...
A method for the analysis of the antimycotic drugs 1-[(5-chloro-2-benzofuranyl)(2-chlorophenyl)methyl]-1H-imidazole, 1-[(5-bromo-2-benzofuranyl)phenylmethyl]-1H-imidazole and bifonazole in rabbit plasma, employing gas chromatography—mass spectrometry with selected-ion monitoring, was developed....
[4-14C]Estrone was injected into three mature Rhode Island hens. Radioactive steroids and steroid conjugates were recovered from the urine on columns of Amberlite XAD-2 and fractionated on columns of DEAE-Sephadex A-25 in a NaCl gradient. Two minor less polar radioactive fractions (I and II) wer...
BackgroundOvercorrection of plasma sodium in severe hyponatremia is associated with osmotic demyelination syndrome. Desmopressin (DDAVP) can prevent overcorrection of plasma sodium in hyponatremia. The objective of this study was to compare outcomes in hyponatremia according to DDAVP usage.
BackgroundClinical benefit has not been evaluated much in patients with nocturia.
Antiplatelet therapy at the time of spontaneous intracerebral hemorrhage (sICH) may increase risk for hemorrhage expansion and mortality. Current guidelines recommend considering a single dose of desmopressin in sICH associated with cyclooxygenase-1 inhibitors or adenosine diphosphate receptor i...
SummaryIntroductionThe nocturnal polyuria is considered a significant predictive value for response to desmopressin. The cutoff value useful to define nocturnal polyuria is still a matter of debate. Moreover, it is current notion that maximal voided volume (MVV) could be used as a predictor for ...
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