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Synthesis and biological evaluation of tricyclic guanidine analogues of batzelladine K for antimalarial, antileishmanial, antibacterial, antifungal and anti-HIV activities
Chemical Biology & Drug Design ( IF 3.2 ) Pub Date : 2012-06-15 , DOI: 10.1111/j.1747-0285.2012.01427.x
Nafees Ahmed 1 , Keyur G Brahmbhatt 1 , Shabana I Khan 1 , Melissa Jacob 1 , Babu L Tekwani 1 , Sudeep Sabde 1 , Debashis Mitra 1 , Inder Pal Singh 1 , Ikhlas A Khan 1 , Kamlesh K Bhutani 1
Affiliation  

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:


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14h20l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12c14c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12c14c14i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。
更新日期:2012-06-15
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