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N-取代 2-氨基苯并噻唑的抗感染和除草活性。

Anti-infective and herbicidal activity of N-substituted 2-aminobenzothiazoles.

机构信息

Department of Chemical Drugs, Faculty of Pharmacy, University of Veterinary and Pharmaceutical Sciences, Palackeho 1/3, 612 42 Brno, Czech Republic.

出版信息

Bioorg Med Chem. 2012 Dec 15;20(24):7059-68. doi: 10.1016/j.bmc.2012.10.007. Epub 2012 Oct 17.

Abstract

In this study, a series of N-substituted 2-aminobenzothiazoles was prepared according to a recently developed method. Twelve compounds were tested for their activity related to the inhibition of photosynthetic electron transport (PET) in spinach (Spinacia oleracea L.) chloroplasts. Primary in vitro screening of the discussed compounds was also performed against fungal, bacterial and mycobacterial species. The biological activities of some compounds were comparable or higher than the standards phenoxymethylpenicillin or pyrazinamide. The most effective compounds demonstrated insignificant toxicity against the human monocytic leukemia THP-1 cell line. For all compounds, the structure-activity relationships are discussed.

摘要

在这项研究中,根据最近开发的方法,制备了一系列 N-取代的 2-氨基苯并噻唑。测试了 12 种化合物在抑制菠菜(Spinacia oleracea L.)叶绿体光合作用电子传递(PET)方面的活性。还对所讨论的化合物进行了针对真菌、细菌和分枝杆菌的初步体外筛选。一些化合物的生物活性与标准苯氧甲基青霉素或吡嗪酰胺相当或更高。最有效的化合物对人单核细胞白血病 THP-1 细胞系的毒性可忽略不计。对于所有化合物,都讨论了结构-活性关系。

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