Chemical synthesis, spectroscopic analysis, antioxidant, and antimicrobial activities of some hydrazones derived from 4-fluorobenzohydrazide
TL;DR: In this paper, the synthesis of substituted 2,6-diphenylpiperidin-4-one with 4-fluorobenzhydrazide is discussed.
About: This article is published in Materials Today: Proceedings.The article was published on 2021-11-25 and is currently open access. It has received None citations till now. The article focuses on the topics: Carbon-13 NMR & Proton NMR.
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TL;DR: There was good interlaboratory agreement with amphotericin B, fluconazole, and flucytosine; ketoconazole gave more variable results.
Abstract: A collaborative comparison of macro- and microdilution antifungal susceptibility tests was performed in five laboratories MICs of amphotericin B, fluconazole, flucytosine, and ketoconazole were determined in all five centers against 95 coded isolates of Candida spp, Cryptococcus neoformans, and Torulopsis glabrata A standard protocol with the following National Committee for Clinical Laboratory Standards Subcommittee on Antifungal Susceptibility Testing recommendations was used: an inoculum standardized by spectrophotometer, buffered (RPMI 1640) medium (pH 70), incubation at 35 degrees C, and an additive drug dilution procedure Two inoculum sizes were tested (1 x 10(4) to 5 x 10(3) to 25 x 10(3) CFU/ml) and three scoring criteria were evaluated for MIC endpoint determinations, which were scored as 0 (optically clear), < or = 1 (slightly hazy turbidity), and < or = 2 (prominent decrease in turbidity compared with that of the growth control) Overall intra- and interlaboratory reproducibility was optimal with the low-density inoculum, the second-day readings, and MICs scored as either 1 or 2 The microdilution MICs demonstrated interlaboratory agreement with most of the four drugs higher than or similar to that of the macrodilution MICs In general, there was good interlaboratory agreement with amphotericin B, fluconazole, and flucytosine; ketoconazole gave more variable results
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227 citations
TL;DR: In this paper, a dual autoclaving-retrogradation treatment was designed for preparing resistant starch from four rice cultivars and its impact on invitro digestibility, pasting, thermal and structural properties was determined.
174 citations
TL;DR: In vitro analysis of antifungal activity of these agents would also allow for the comparison between different antimycotics, which in turn may clarify the reasons for lack of clinical response or serve as an effective therapy for patients with chronic infection.
Abstract: Summary Background With the development of newer antifungal agents with activity against both yeasts and filamentous fungi, there is an increased need to develop and standardize in vitro assays that will evaluate the activity of antimycotics against filamentous fungi. In vitro analysis of antifungal activity of these agents would also allow for the comparison between different antimycotics, which in turn may clarify the reasons for lack of clinical response or serve as an effective therapy for patients with chronic infection.
Objectives To determine the in vitro susceptibility of fungal organisms to ciclopirox, terbinafine, ketoconazole and itraconazole and to evaluate the in vitro activity and mode of interaction of ciclopirox in combination with either terbinafine or itraconazole.
Materials and methods In the minimum inhibitory concentration (MIC) study 133 strains were evaluated, including dermatophytes (110 strains; 98 from Trichophyton spp.), Candida spp. (14 strains) and nondermatophyte moulds (nine strains). In vitro susceptibility testing was conducted in microbroth dilutions based on the National Committee for Clinical Laboratory Standards (NCCLS) M27-A proposed standard. The testing MIC ranges were 0·003–2 μg mL−1 for ciclopirox and terbinafine, and 0·06–32 μg mL−1 for itraconazole and ketoconazole. For inoculum preparation, dermatophytes were grown on Heinz oatmeal cereal agar slants. Inoculum suspensions of dermatophytes were diluted in RPMI 1640 (Sigma-Aldrich) with the desired final concentration being 2–5 × 103 c.f.u. mL−1. Once inoculated, the microdilution plates were set up according to the NCCLS M27-A method, incubated at 35 °C, and read visually following 7 days of incubation. For azole agents, the MIC was the lowest concentration showing 80% growth inhibition; for terbinafine and ciclopirox, the MIC was the lowest concentration showing 100% growth inhibition. In the synergy studies, 29 strains from nondermatophyte species were evaluated using a checkerboard microdilution method. The concentrations tested were: 0 and 0·06–32 μg mL−1 for itraconazole, and 0 and 0·003–4 μg mL−1 for both terbinafine and ciclopirox. Modes of interaction between drugs were classified as synergism, additivism, antagonism or indifference based on fractional inhibitory concentration index values (FIC index). Synergism was defined as an FIC index of ≤ 0·50, additivity as an FIC index of ≤ 1·0, and antagonism as an FIC index of ≥ 2·0. The drug combination was interpreted as indifferent if neither of the drugs had any visible effect on the presence of the other drug.
Results In the MIC study, the dermatophyte MIC values (μg mL−1) (mean ± SEM) were: ciclopirox (0·04 ± 0·02), terbinafine (0·04 ± 0·23), itraconazole (2·28 ± 7·42) and ketoconazole (0·83 ± 1·99). The yeast MIC values (μg mL−1) (mean ± SEM) were: ciclopirox (0·05 ± 0·02), terbinafine (1·77 ± 0·58), itraconazole (0·18 ± 0·27) and ketoconazole (0·56 ± 0·60). The non-dermatophyte fungi MIC values (μg mL−1) (mean ± SEM) were: ciclopirox (1·04 ± 2·62), terbinafine (1·04 ± 0·95), itraconazole (17·87 ± 16·75) and ketoconazole (10·69 ± 13·09). In the synergy study, with ciclopirox in combination with terbinafine, mainly a synergistic or additive reaction was observed; there were no cases of antagonism. For ciclopirox in combination with itraconazole, there were some instances of additivism or synergism, with indifference in the majority of instances; there were no cases of antagonism.
Conclusions In vitro susceptibility testing indicates that ciclopirox may have a broad antimicrobial profile including dermatophytes, yeasts and other nondermatophytes. Terbinafine is extremely potent against dermatophytes. In vitro evaluation of activity of ciclopirox and terbinafine suggests many instances of synergy or additivism; for ciclopirox and itraconazole there may be indifference, synergy or additivism.
167 citations