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PubMed2006

Quantum chemical study of the inhibitive properties of 2-pyridyl-azoles.

Four molecules that have been proven to act as corrosion inhibitors of mild steel in acidic media are studied. The inhibitive efficiency of these molecules is explained by means of electronic structure calculations of the protonated species that seem to represent better the actual situation of the experimental conditions. By assuming that the interaction between the inhibitor and the metallic surface occurs through donation and back-donation, it is shown, with a simple charge transfer model, that the interaction energy is favored when hardness increases, in agreement with the experimentally observed inhibition efficiencies. A local analysis with Hirshfeld condensed Fukui functions, and local Fukui functions, provides further support to the donation and back-donation mechanism.

Journal Article↗
PubMed2003

Acetylenic acids inhibiting azole-resistant Candida albicans from Pentagonia gigantifolia.

Antifungal bioassay-guided isolation of the ethanol extract of the roots of Pentagonia gigantifolia yielded 6-octadecynoic acid (1) and the new 6-nonadecynoic acid (2). Compounds 1 and 2 inhibited the growth of fluconazole-susceptible and -resistant Candida albicans strains. Their antifungal potencies were comparable to those of amphotericin B and fluconazole. Of particular significance is the low cytotoxicity and specific activity of 1 and 2 against C. albicans.

Amphotericin B↗
PubMed2005

On the utility of the azido transfer protocol: synthesis of 2- and 5-azido N-methylimidazoles, 1,3-thiazoles and N-methylpyrazole and their conversion to triazole-azole bisheteroaryls.

The azido transfer procedure of heteroaryllithium and tosyl azide was used to synthesize selected 2- and 5-azidoazoles. This procedure, which is based on the fragmentation of the appropriate lithium triazene salts 1a-7a, successfully afforded 2-azido-N-methylimidazole 1, 2-azido-1,3-thiazole 2, 2-azidobenzo-1,3-thiazole 3, 5-azido-N-methylpyrazole 4, 5-azido-N-methylimidazole 6[via 2-(trimethylsilyl)-5-azido-N-methylimidazole 5], and 5-azido-1,3-thiazole 7 (via 5-lithio-1,3-thiazole), but attempts to prepare 5-azido-2-(trimethylsilyl)-1,3-thiazole 8 from the corresponding triazene 7a failed, affording only the desilylated azide in poor yield. Azides - underwent 1,3-dipolar cycloaddition when mixed with neat (trimethylsilyl)acetylene, giving 1-heteroaryl-4-trimethylsilyl-1,2,3-triazoles 1b-7b generally in very high yields.

Journal Article↗
PubMed2006

Kinetics and mechanism of the reactions of Pd(II) complexes with azoles and diazines. Crystal structure of [Pd(bpma)(H2O)](ClO4)2.2H2O.

Substitution reactions of the complexes [Pd(bpma)(H2O)]2+, [Pd(bpma)Cl]+, [Pd(dien)(H2O)]2+ and [Pd(dien)Cl]+, where bpma = bis(2-pyridylmethyl)amine and dien = diethylentriamine or 1,5-diamino-3-azapentane, with some nitrogen-donor ligands such as triazole, pyrazole, pyrimidine, pyrazine and pyridazine, were studied in an aqueous 0.10 M NaClO4 at pH 2.8 using variable-temperature and -pressure stopped-flow spectrophotometry. The second-order rate constants indicate that the Pd(II) complexes of bpma, viz. [Pd(bpma)(H2O)]2+ and [Pd(bpma)Cl]+, are more reactive than the complexes of dien, viz. [Pd(dien)(H2O)]2+ and [Pd(dien)Cl]+. Also, the aqua complexes, [Pd(bpma)(H2O)]2+ and [Pd(dien)(H2O)]2+, are much more reactive than the corresponding chloro complexes. The most reactive nucleophile of the five-membered rings is triazole and for the six-membered rings the most reactive one is pyridazine. Activation parameters were determined for all reactions and the negative entropies and volumes of activation (Delta S++, Delta V++) support an associative ligand substitution mechanism. The crystal structure of [Pd(bpma)(H2O)](ClO4)2.2H2O was determined by X-ray diffraction. Crystals are monoclinic with the space group P2(1)/c. The coordination geometry of [Pd(bpma)(H2O)]2+ is distorted square-planar. The Pd-N (central) bond distance, 1.958(5) A, is shorter than the other two Pd-N distances, 2.007(5) and 2.009(5) A. The Pd-O distance is 2.043(5) A.

Journal Article↗
PubMed2003

Disseminated aspergillosis due to Aspergillus flavus in an experimental model: efficacy of azole therapy.

The aim of this investigation was to create a reproducible experimental model of disseminated Aspergillus flavus aspergillosis, and to compare the relative therapeutic efficacies of itraconazole and fluconazole in this model. Temporarily immunosuppressed male Wistar rats received intravenous challenge by A. flavus conidia. Treatment was initiated 24 h later with oral itraconazole (1 mg kg-1 BW day-1), oral fluconazole (1 mg kg-1 BW day-1) or excipient only (infected-untreated rats); this was continued for 10 days. At this time, although 100% mortality had occurred among all infected-untreated rats, no mortality was noted among the control-uninfected, infected-itraconazole-treated or infected-fluconazole-treated rats. After killing, essential organs were processed for microbiological and histopathological studies. Aspergillus flavus was recovered in high colony counts from the organs of infected-untreated rats (lungs > liver > brain > kidneys), but in significantly lower colony counts, or not at all, from the organs of itraconazole-treated and fluconazole-treated rats. Histopathological alterations were pronounced in tissues of infected-untreated rats, but less so in treated rats. These data suggest that administration of itraconazole or fluconazole sufficiently early may prevent, or retard, progression of lesions in disseminated aspergillosis.

Administration, Oral↗
PubMed1996

Role of azoles in antifungal therapy.

The addition of itraconazole and fluconazole to the antifungal armamentarium has resulted in less toxic, easily administered therapy for both endemic and opportunistic mycoses. Itraconazole has become the treatment of choice for most patients with mild-to-moderate histoplasmosis, blastomycosis, and sporotrichosis. Coccidioidomycosis is effectively treated with either itraconazole or fluconazole; fluconazole has become the drug of choice for the treatment of coccidioidal meningitis. In several large cooperative trials, fluconazole has been shown to have a useful role in the treatment of patients with candidemia, localized forms of mucocutaneous and visceral candidiasis, and cryptococcal meningitis.

Antifungal Agents↗
PubMed1985

New azole compounds: vibunazole (Bay n7133) and Bay L9139, compared with ketoconazole in the therapy of systemic candidosis and in pharmacokinetic studies, in mice.

Ketoconazole, a new imidazole: Bay L9139, and a new triazole: vibunazole (Bay n7133) were compared in therapy of systemic candidosis. CD-1 male mice were challenged with Candida albicans intravenously (greater than LD80), and treated twice a day, orally, for one month. The isolate of Can. albicans used, and isolates obtained after treatment with the antifungals, were susceptible to all three drugs (MICs less than or equal to 0.5 mg/l). No drug was lethal to uninfected mice in doses of 200 mg/kg/day for one month. With therapy started on the day after infection, all three drugs at 50 or 100 mg/kg/day prolonged survival, compared with controls (P less than 0.05), with ketoconazole slightly superior to the other two drugs, but none did so at 25 mg/kg/day. At 200 mg/kg/day ketoconazole and vibunazole were protective, but L9139 was not, and this suggested synergistic toxicity of L9139 with Can. albicans infection, at this dose. With treatment begun on day 4, ketoconazole prolonged survival (P less than 0.005) at 200 or 100 mg/kg/day compared with controls, but ketoconazole at 10-50 mg/kg/day, and vibunazole and L9139 at 10-200 mg/kg/day were ineffective. Survivors had renal lesions and culture-proven residual infection. Pharmacokinetic studies indicated lower peak vibunazole and 9139 serum concentrations, and reduced area-under-curve (AUC), after 26 days of treatment, as against single dose administration. The relative inefficacy of vibunazole and L9139 appears to be related to unfavourable pharmacokinetic properties with continued administration.

Animals↗
PubMed1988

Effects of azole antifungals in vitro on host/parasite interactions relevant to Candida infections.

Clotrimazole, fluconazole, itraconazole and ketoconazole were tested for their influence on three aspects of host/parasite interactions in the context of Candida infections. None of clotrimazole, itraconazole or ketoconazole had any effect on the adherence of C. albicans to vaginal epithelial cells, in vitro, regardless of whether the drugs were used to pretreat the fungi or the vaginal cells or were added to the fungus/vaginal cell mixture. Clotrimazole pretreatment of polymorphonuclear leucocytes led to a marked suppression of their ability to phagocytose and kill C. albicans, but fluconazole and ketoconazole had no similar effect. None of these three antifungals affected phagocytosis or killing when they were added to the leucocyte candida mixture or when used to pretreat the fungi. Clotrimazole and ketoconazole both reduced proliferative responses of lymphocyte suspensions to mitogens but fluconazole showed no anti-lymphocyte effect. This difference in action against lymphocytes may help to explain the known disparity between the antifungal effects of fluconazole and ketoconazole against C. albicans in vivo and against experimental candida infections in vitro. Clotrimazole effected a suppression of ATP concentrations in lymphocytes but fluconazole and ketoconazole had no similar effects.

Antifungal Agents↗