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Mini-Reviews in Medicinal Chemistry


ISSN (Print): 1389-5575
ISSN (Online): 1875-5607

A Critical View on Antimalarial Endoperoxide QSAR Studies

Author(s): R. R. Teixeira, J. W. de M. Carneiro, M. T. de Araujo and A. G. Taranto

Volume 12, Issue 6, 2012

Page: [562 - 572] Pages: 11

DOI: 10.2174/138955712800493852

Price: $65


Malaria is one of the most dangerous diseases in developing countries. The chemotherapy of malaria has been based on drugs developed more than half a century ago. These drugs are continuously losing their efficacy, mainly due to multi-drug resistance developed by the malaria-causing parasite. In the last three decades, artemisinin and artemisinin-like compounds have proven to be efficient alternatives to the chemotherapeutic control of malaria. These facts have led to an increasing interest in the development of Quantitative Structure Activity Relantioship (QSAR) models for these compounds. This work presents a critical view on some QSAR models, and shows that, due to lack of a rigorous selection of the descriptors entering the models, most of them are unable to accurately indicate the molecular cause of biological activity. Some reasons for the weakness of the published models are discussed.

Keywords: QSAR, malaria, artemisinin, endoperoxide, mechanism of action, mefloquine, chloroquine, Plasmodium falciparum, artemisinin, Plasmodium sp, lipophilic, glutathione-S-transferase, sulfotransferases

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