کد مقاله کد نشریه سال انتشار مقاله انگلیسی نسخه تمام متن
1360910 981452 2008 11 صفحه PDF دانلود رایگان
عنوان انگلیسی مقاله ISI
Design, synthesis, and application of novel triclosan prodrugs as potential antimalarial and antibacterial agents
موضوعات مرتبط
مهندسی و علوم پایه شیمی شیمی آلی
پیش نمایش صفحه اول مقاله
Design, synthesis, and application of novel triclosan prodrugs as potential antimalarial and antibacterial agents
چکیده انگلیسی

A number of new triclosan-conjugated analogs bearing biodegradable ester linkage have been synthesized, characterized and evaluated for their antimalarial and antibacterial activities. Many of these compounds exhibit good inhibition against Plasmodium falciparum and Escherichia coli. Among them tertiary amine containing triclosan-conjugated prodrug (5) inhibited both P. falciparum (IC50; 0.62 μM) and E. coli (IC50; 0.26 μM) at lower concentrations as compared to triclosan. Owing to the presence of a cleavable ester moiety, these new prodrugs are hydrolyzed under physiological conditions and parent molecule, triclosan, is released. Further, introduction of tertiary/quaternary functionality increases their cellular uptake. These properties impart them with higher potency to their antimalarial as well as antibacterial activities. The best compound among them 5 shows close to four-fold enhanced activities against P. falciparum and E. coli cultures as compared to triclosan.

Novel triclosan-conjugated analogs bearing biodegradable ester linkage have been synthesized and evaluated for their antimalarial and antibacterial activities against Plasmodium falciparum and Escherichia coli. Many of the compounds were found to possess potent activities against P. falciparum and E. coli cultures.Figure optionsDownload as PowerPoint slide

ناشر
Database: Elsevier - ScienceDirect (ساینس دایرکت)
Journal: Bioorganic & Medicinal Chemistry - Volume 16, Issue 10, 15 May 2008, Pages 5536–5546
نویسندگان
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