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Issue 6, 2013
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Meridianin G and its analogs as antimalarial agents

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Abstract

The marine-derived indole alkaloids meridianin C and G and their N1-substituted and C-ring modified analogs were synthesized and screened for antiprotozoal and antimicrobial activities. Meridianin C and G showed antimalarial activity against both chloroquine-resistant (D6) as well as sensitive (W2) clones of Plasmodium falciparum with IC50 values in the range of 4.4 to 14.4 μM. Meridianin G showed better activity against the W2 clone, showing a higher selectivity index >24.1. Among the analogs, N1-morpholinoyl meridianin C analog displayed antimalarial activity against both clones, showing selectivity indices up to 25.1. Meridianin C along with a few other analogs showed weak to moderate antileishmanial activity against Leishmania donovani promastigotes, the best analog being a C-ring modified 5-iodo meridianin showing an IC50 of 9.17 μM. A few compounds also showed mild antibacterial activity against Staphylococcus aureus and methicillin-resistant S. aureus, and antifungal activity against Cryptococcus neoformans.

Graphical abstract: Meridianin G and its analogs as antimalarial agents

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Publication details

The article was received on 29 Mar 2013, accepted on 09 Apr 2013 and first published on 16 Apr 2013


Article type: Concise Article
DOI: 10.1039/C3MD00097D
Citation: Med. Chem. Commun., 2013,4, 1042-1048
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    Meridianin G and its analogs as antimalarial agents

    S. B. Bharate, R. R. Yadav, S. I. Khan, B. L. Tekwani, M. R. Jacob, I. A. Khan and R. A. Vishwakarma, Med. Chem. Commun., 2013, 4, 1042
    DOI: 10.1039/C3MD00097D

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