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 的三环胍类似物的合成和生物学评价，用于抗疟、抗寄生虫、抗菌、抗真菌和抗 HIV 活性

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（多诺瓦尼利什曼原虫）、抗菌（细菌和真菌组）、抗病毒（HIV-1）活性。类似物14h和20l对氯喹敏感的 D6 菌株具有潜在的抗疟活性，IC ₅₀为 1.25 和 0.88 μM，对氯喹耐药的 W2 菌株的 IC ₅₀分别为 1.64 和 1.07 μM。具有壬基取代的类似物12c和14c显示出最有效的抗利什曼虫活性，IC _{50 为}2.39 和 2.78 μM，IC 为₉₀分别为 11.27 和 12.76 μM。三种类似物12c、14c和14i对各种病原细菌和真菌最有效，IC ₅₀ <3.02 μM 和 MIC/MBC/MFC <6 μM。在三环上具有戊基和甲基取代基的类似物20l显示出对所有病原体的有希望的活性。然而，没有发现对 HIV-1 有活性。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。