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2011年全国药物化学学术会议——药物的源头创新

作者： guri lv damu School of Chemistry and Chemical Engineering Southwest University Postdoctoral fellow from Indian Institute of Chemical Technology（IICT） India

＜正＞Coumarins and their derivatives with typical 1,2-benzopyrone framework have been widely used in the field of bromatology,material and supramolecular chemistry as well as pharmacochemistry. Especially in medicinal chemistry,coumarin compounds have attracted great attention because of their wide biological *** diseases have been increasingly serious threatens to human

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Synthesis and Antimicrobial Evaluation of Novel Naphthalimide-derived Coumarin Triazolium#

Synthesis and Antimicrobial Evaluation of Novel Naphthalimid...

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2011年全国药物化学学术会议——药物的源头创新

作者： guri lv damu School of Chemistry and Chemical Engineering Southwest University Postdoctoral fellow from Indian Institute of Chemical Technology（IICT） India

＜正＞Coumarins have been paid special attentions due to their extensive potential application in medicinal Chemistry,agrochemical aspects,perfume and supramolecular *** in pharmaceutical sciences,many coumarin derivatives have already been widely used in clinic. Recently,a lot of researches showed that the introduction of some nitrogen-containing

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Researches in Thiazoles as Enzyme and Receptor Inhibitors

Researches in Thiazoles as Enzyme and Receptor Inhibitors

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2011年全国药物化学学术会议——药物的源头创新

作者： guri lv damu School of Chemistry and Chemical Engineering Southwest University Postdoctoral fellow from Indian Institute of Chemical Technology（IICT） India

＜正＞Enzymes and receptors as targets for drug designs are one of the most active fields in medicinal *** with intensive studies on the role of enzymes and receptors in the disease pathogenesis and metabolic process,...

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A series of naphthalimide azoles: Design, synthesis and bioactive evaluation as potential antimicrobial agents

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Science China Chemistry 2013年第7期56卷 952-969页

作者： damu guri L. V. WANG QingPeng ZHANG HuiZhen ZHANG YiYi lv JingSong ZHOU ChengHe School of Chemistry and Chemical Engineering Southwest University School of Chemistry and Chemical Engineering Bijie University

A series of naphthalimide azoles as potential antibacterial and antifungal agents were conveniently and efficiently synthesized starting from commercially available 6-bromobenzo[de]isochromene-l,3-dione. All the new compounds were characterized by NMR, IR, MS and HRMS spectra. Their antimicrobial activities were evaluated against four Gram-positive bacteria, four Gram-negative bacteria and two fungi using two-fold serial dilution technique. The biological assay indicated that most of the prepared compounds exhibited inhibition to the tested strains. In particular, the triazolium derivatives not only gave higher ef- ficacy than their corresponding precursory azoles, but also demonstrated comparable or even better potency than the reference drugs Chloromycin, Orbifloxacin and Fluconazole. Some factors including structural fragments, pH and ClogP values of the target molecules were also preliminarily discussed.

关键词： naphthalimide triazole imidazole triazolium imidazolium thiol thione antibacterial antifungal antimicrobial

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