In Vitro Selection and In Vivo Efficacy Piperazine- and Alkanediamide-Linked Bisbenzamidines against Pneumocystis Pneumonia in Mice  

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Jenis: Article from Journal - ilmiah internasional
Dalam koleksi: Antimicrobial Agents and Chemotherapy vol. 50 no. 07 (Jul. 2006), page 2337.
Topik: Piperazine; Alkanediamide; Pneumocystis Pneumonia

Ketersediaan

Perpustakaan FK Nomor Panggil: A21.K, A21.K.2006.03 Non-tandon: 3 (dapat dipinjam: 0) Tandon: tidak ada

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Isi artikel

Bisbenzamidines, such as pentamidine isethionate, are aromatic dicationic compounds that are active against Pneumocystis and other microbes but are oftentimes toxic to the host. To identify potential anti-Pneumocystis agents, we synthesized bisbenzamidine derivatives in which the parent compound pentamidine was modified by 1,4-piperazinediyl, alkanediamide, or 1,3-phenylenediamide moiety as the central linker. Several of the compounds were more active against P. carinii and less toxic than pentamidine in cytotoxicity assays. For this study, we evaluated 9 bisbenzamidine derivatives representing a range of in vitro activities, from highly active to inactive, for the treatment of pneumocystosis in an immunosuppressed mouse model.Thus, the selection of highly active compounds from in vitro cytotoxicity assays was predictive of activity in the mouse model of Pneumocystis pneumonia. We conclude that a number of these bisbenzamidine compounds, aspecially compound 100, may show promise as new anti-Pneumocystis drugs.

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