Synthesis and biological evaluation of tricyclic guanidine analogues of batzelladine K for antimalarial, antileishmanial, antibacterial, antifungal, and anti-HIV activities

Nafees Ahmed, Keyur G Brahmbhatt, Shabana Khan, Melissa Jacob, Babu Lal Tekwani, Sudeep Sabde, Debashis Mitra, Inder Pal Singh, Ikhlas Khan, Kamlesh Kumar Bhutani

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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?m and chloroquine-resistant W2 strain with IC50 1.64 and 1.07?m, respectively. Analogues 12c and 14c having nonyl substitution showed the most potent antileishmanial activity with IC50 2.39 and 2.78?m and IC90 11.27 and 12.76?m, respectively. Three analogues 12c, 14c, and 14i were the most active against various pathogenic bacteria and fungi with IC50
Original languageEnglish
Pages (from-to)491 - 498
Number of pages8
JournalChemical Biology & Drug Design
Issue number4
Publication statusPublished - 2013

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