Polarographic and spectrophotometric behaviour of some aminoazole derivatives

The structure of differently substituted azole amines is receiving considerable interest [1,3] but the structure of aminoisoxazolnes has seldom been adequately investigated. Literature inspection reveales that only few 3-amino-isoxazolones have been synthesised. Elnagdi et al [4] described the synthesis of 5- amino - 4- arylhydrazono-1,2 oxazole-3- ones [1] and their isomeric 3- amino-4- arylhydrazono-l,2-oxazole-5- ones [2]. However, the structure of these isoxazolone derivaties have not been exclusively defined. In conjunction with any investigation aiming to test the potential of the above compounds as dyes and precursors in dye synthesis, better understanding of the structure of these compounds seemed to be of value. In the present work, the polarographic behaviours of compounds [1] and [2] studies and pK values are calculated, to get insight into the nature of the various tautomeric structures of [1] and [2] their electroreduction in alcoholic buffered media covering a wide range of pH

Resistance of candida species isolated form differnt pathological lesions to azole derivatives

Over the last three decades a variety of drugs have been developed for treatment of candidal infections, of these azoles have achieved a great impact, but azole resistance have been recently implicated as a cause of treatment failure in patients with candidal infections. So, the aim of this study is to test resistance of candidal isolates of different clinical samples to azoles, and to test combined azole preparations to detect synergistic actions of such drugs when used topically or systematically. To achieve the aim, 123 clinically diagnosed cases of candidiasis were sampled, examined by DM, count culture and culture on SDA, the 90 yielded isolates were identified by rapid Candifast identification method. Azole resistance was tested by a resistogram microtube commercial method and also by YNB agar-azole diluted method for more accuracy. The tested azoles were Clotrimazole [CMZ], Ketoconazole [KTZ], Miconazole [MCZ], Econazole [ECZ], Itraconazole [ICZ], Tioconazole [TCZ] and Fluconazole [FCZ]. In addition to C. albicans, other Candida species now emerge as pathogens. Resistance to topically used and systemically used azoles is high. KTZ is the most effective one [16.7, 25.6 resistant strains by the 2 methods at 15.6 ug/ml]. Nearly 1/3 of strains were resistant to azoles used at 7.8 ug/ml concentrations. Many combined topical azoles showed synergistic effect while the only combination of systemically used azoles that showed synergism was KTZ+FCZ

Studies on heterocyclic nitrogen compounds, new azoles from benzo- [G]-1, 2, 3, 4-tetra-hydroquinoline-4, 5, 10-trione derivatives

Pyrazoline, isoxazoline. pyrimidine and pyrimidinethione derivatives have been reported as highly potent agent against fungi and bacteria[1-6] As a result of our interest to prepare a new and microbial active azoles [7-10], we report here the synthesis of new azoles and pyrimidinone derivatives starting from benzo- [G] -4-chloro-l,2-dihydroquinolinoquinone-3-carboxaldehyde [2]. Formylation of benzo-[G] 1,2,3,4-tetrahydroquinoline 4,5, 10-trione [l][11] via Vilsmeier reagent [POC13/DMF] afforded benzo-[G]-4-ch1oro-l, 2-, dihydroquinolinoquinone-3-carboxaldehyde [2]. The 1HNMR spectra of [2] have shown a singlet signal at sigma 10.0 pmm due to proton of the formyl group and its mass spectra showed clear isotopic effect. Condensation of the formylated compound [2] and 4-substituted acetophenone in alkaline ethanol produced the corresponding alpha, beta unsaturated compounds [3 a-c].[1]H NMR. Spectra of the compourds [3a-c] showed the disappearance of the formyl proton at sigma10.0 ppm, meanwhile two doublets are observed around sigma 5 .8-6.2 ppm, for protons at conjugated double bond. Cycloaddition reaction of [3a-c] and hydrazine hydrate in presence of acetic acid, phenylhydrazine in catalytic amounts of piperidine, hydroxylamine hydro chloride in alkaline ethanol, urea and/or thiourea in presence of 5NHC1 afforded the corresponding pyrazolines [4a,b; 4d, e and 4g, h], isoxazolines [4c; 4f and 4i] pyrimidinone [5a; 5c and 5e] and/or pyrimidinethione [5b; 5c and 5f], respectively. The chemical structure of these new compounds were established based on IR, [1] H-NMR and mass spectra, as well as their elemental analysis [c.f. tables 1,2]