Letters in Drug Design & Discovery

Atta-ur-Rahman  , FRS
Honorary Life Fellow
Kings College
University of Cambridge
Cambridge
UK
Email: lddd@benthamscience.org

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In Vivo Assessment of Antileishmanial Property of 4-(4,4,8-Trimethyl-7- oxo-3-oxabicyclo[3.3.1]non-2-yl)-benzoic Acid Methyl Ester, an Oxabicyclo[ 3.3.1]nonanones

Author(s): Prakash Saudagar, Shyam Lal Mudavath, Pipas Saha, Anil K. Saikia, Shyam Sundar and Vikash Kumar Dubey

Affiliation: Department of Biotechnology and Department of Chemistry, Indian Institute of Technology Guwahati, Assam, India- 781039.

Keywords: Drug design, In vivo assessment, Leishmaniasis, Oxabicyclo[3.3.1]nonanones, Toxicity.

Graphical Abstract:


Abstract:

The high toxicity and the growing resistance are the major drawbacks of available antileishmanials. Our previous in vitro studies have identified oxabicyclo[3.3.1]nonanones as antileishmanial agents that act on the redox enzymes of the parasite. In the current study, antileishmanial activity of 4-(4,4,8-trimethyl-7-oxo-3-oxabicyclo[3.3.1]non-2-yl)- benzoic acid methyl ester (PS 203) the most potent oxabicyclo[3.3.1]nonanone identified in our previous study is evaluated using the hamster model. There was 77.29 ± 3.0 % inhibition of parasite growth observed after a 5-day treatment of 5 mg/kg body weight dose. Further, the in vivo toxicity study of the compound in Swiss albino mice revealed no hepatic or renal toxicity.

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Article Details

VOLUME: 11
ISSUE: 7
Page: [937 - 939]
Pages: 3
DOI: 10.2174/1570180811666140423203826