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Protective effect of fructose-1-6-diphosphate against gram-negative experimental infections in mice
No full textSTUDIES ON ANTICANDIDA AGENTS WITH A PYRROLE MOIETY - SYNTHESIS AND MICROBIOLOGICAL ACTIVITY OF SOME 3-AMINOMETHYL-1,5-DIARYL-2-METHYL-PYRROLE DERIVATIVES
No full textResearches on antibacterial and antifungal agents, XIV: Thiophene analogues of bifonazole
No full textSome thiophene analogues of bifonazole have been synthesized by standard procedures and their antifungal activity has been tested against Candida albicans. Among test derivatives bipbenyl-4-yl-5-chloro-thien-2-ylimidazol-1-ylmethane and its 5-deschlorothien-2-yl analogue resulted to be the most active. Their antifungal potency was almost comparable to that of control substances, such as miconazole, ketoconazole, and bifonazole. Replacement of benzene by the Pyrrole ring in the biphenyl portion retained almost quantitatively the antifungal activity, whereas substitution with other azoles and with nitrogen alicyclic rings led always to less potent derivatives
Antifungal agents. III. Naphthyl and thienyl derivatives of 1H-imidazol-1-yl-4-phenyl-1H-pyrrol-3-ylmethane.
No full textThe in vitro antifungal activities of some naphthyl and thienyl derivatives of 1H-imidazol-1-yl-4-phenyl-1H-pyrrol-3-ylmethane against Candida albicans and Candida spp are reported. The title derivatives were prepared starting from proper arylstirylketones, which were reacted with tosylmethylisocyanide (Tos-MIC) to afford the related 4-phenyl-1H-pyrrol-3-yl aryl ketones. Reduction of ketones to the corresponding carbinols followed by treatment of the last compounds with 1,1'-carbonyldiimidazole (CDI) gave the title imidazoles. The related N-methylpyrrole derivatives are also describe
Antifungal Agents. 5. Chloro and Amino Derivatives of 1,2-Diaryl-1-(1H-imidazol-1-yl)ethane with Potent Antifungal Activities.
No full textResearches on Antibacterial and Antifungal Agents. XV. 3-Aryl-4-[a-(1H-imidazol-1-yl)benzyl]pyrroles with Potent Antifungal Activity.
No full textAntifungal Agents. 9. 3-Aryl-4-[a-(1H-imidazol-1-yl)arylmethyl]pyrroles: A New Class of Potent Anti-Candida Agents.
No full textA new class of potent antifungal agents, namely, 3-aryl-4-[a-(1H-imidazol-l-yl)arylmethyllpyrroles,
is described. These compounds are related to bifonazole and pyrrolnitrin, two
compounds belonging to the class of antimycotic drugs. The synthesis of the title pyrroles has
been performed starting from 1,3-diaryl-2-propen-l-onews,h ich were reacted with tosylmethyl
isocyanide to give 3-aroyl-4-arylpyrroles. Reduction of the resulting compounds by lithium
aluminum hydride furnished the related alcohols, which were treated with 1,l’-carbonyldiimidazole
to afford the required imidazole derivatives. Forty-four new pyrroles which
incorporate an (arylmethy1)imidazole moiety in the 3-arylpyrrole structure were prepared by
the above procedure and tested in vitro against Candida albicans and Candida spp. Among
test compounds, 10 were found to be highly active against C. albicans. The most active
derivative (27) was twice as potent (MICgo) as bifonazole, and its activity was 4 times greater
than those of miconazole and ketoconazole. The other nine compounds showed antifungal
activity of-the same order of that of bifonazole and were ca. 2 times as active as miconazole
and ketoconazole. Derivatives 21 and 27 tested in vivo against C. albicans A170 were shown to
be highly effective in rabbit skin candidosis. Pharmacological studies on compounds 27 and
other related pyrroles (19, 35, 36, 38, 39, and 49) are in progress to select one of them as a
potential candidate for clinical experiments
ANTIFUNGAL AGENTS .8. SYNTHESIS AND ANTIFUNGAL ACTIVITIES OF BIPYRRYL ANALOGS OF BIFONAZOLE
No full textVarious bipyrryl analogues of bifonazole were synthesized starting from aryl-3-pyrryl-1-imidazolylmethanes. The introduction of a second pyrryl portion was performed by linking an acrylate moiety at 1-position of the pyrrole ring and then by treatment with TosMIC. The bipyrryl esters were hydrolyzed and decarboxylated to afford the required imidazoles. All new imidazole derivatives were tested against Candida albicans and Candida spp using as standard controls miconazole, bifonazole and ketoconazole
Going Beyond Counting First Authors in Author Co-citation Analysis
Full text linkThe present study examines one of the fundamental aspects of author co-citation analysis (ACA) - the way co-citation
counts are defined. Co-citation counting provides the data on which all subsequent statistical analyses and mappings
are based, and we compare ACA results based on two different types of co-citation counting - the traditional type that
only counts the first one among a cited work's authors on the one hand and a non-traditional type that takes into
account the first 5 authors of a cited work on the other hand. Results indicate that the picture produced through this non-traditional author co-citation counting contains more coherent author groups and is therefore considerably clearer. However, this picture represents fewer specialties in the research field being studied than that produced through the traditional first-author co-citation counting when the same number of top-ranked authors is selected and analyzed. Reasons for these effects are discussed
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