Fifty analogues of batzelladine K were synthesized and evaluated for in vitro antimalarial (Plasmodium falciparum), antileishmanial (Leishmania donovani), antimicrobial (panel of bacteria and fungi), antiviral (HIV-1) activities. Analogues 14h and 20l exhibited potential antimalarial activity against chloroquine-sensitive D6 strain with IC₅₀ 1.25 and 0.88 μM and chloroquine-resistant W2 strain with IC₅₀ 1.64 and 1.07 μM, respectively. Analogues 12c and 14c having nonyl substitution showed the most potent antileishmanial activity with IC₅₀ 2.39 and 2.78 μM and IC₉₀ 11.27 and 12.76 μM respectively. Three analogues 12c, 14c and 14i were the most active against various pathogenic bacteria and fungi with IC₅₀ <3.02 μM and MIC/MBC/MFC <6 μM. Analogue 20l having pentyl and methyl substituents on tricycle showed promising activities against all pathogens. However, none was found active against HIV-1. Our study demonstrated that the tricyclic guanidine compounds provide new structral class for broad spectrum activity.

中文翻译：

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Batzelladine K 三环胍类似物的合成及其抗疟、抗利什曼尼、抗菌、抗真菌和抗 HIV 活性的生物学评价


合成了 50 种 batzelladine K 类似物，并评估其体外抗疟（恶性疟原虫）、抗利什曼原虫（杜氏利什曼原虫）、抗菌（细菌和真菌）、抗病毒 (HIV-1) 活性。类似物14h和20l分别对氯喹敏感的D6菌株和氯喹抗性W2菌株表现出潜在的抗疟活性，IC ₅₀ 1.25和0.88μM，IC ₅₀ 1.64和1.07μM。具有壬基取代的类似物12c和14c显示出最有效的抗利什曼活性，IC ₅₀分别为2.39和2.78μM，IC ₉₀ 11.27和12.76μM。三种类似物12c 、 14c和14i对各种病原菌和真菌最有活性，其IC ₅₀ <3 id=59>20l 在三环上具有戊基和甲基取代基，显示出针对所有病原体的有希望的活性。然而，没有发现任何药物具有抗 HIV-1 的活性。我们的研究表明，三环胍化合物为广谱活性提供了新的结构类别。