Journal
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
Volume 22, Issue 14, Pages 4593-4598Publisher
PERGAMON-ELSEVIER SCIENCE LTD
DOI: 10.1016/j.bmcl.2012.05.103
Keywords
Acetylcholinesterase; Species-selectivity; Malaria; Mosquito; Mechanism-based inactivator
Categories
Funding
- National Institutes of Health [AI082581]
- Foundation for the National Institutes of Health through Grand Challenges in Global Health Initiative [GCGH-1497]
- Virginia Tech (the College of Science, the Department of Chemistry, and Fralin Life Science Institute)
Ask authors/readers for more resources
To identify potential human-safe insecticides against the malaria mosquito we undertook an investigation of the structure-activity relationship of aryl methylcarbamates inhibitors of acetylcholinesterase (AChE). Compounds bearing a beta-branched 2-alkoxy or 2-thioalkyl group were found to possess good selectivity for inhibition of Anopheles gambiae AChE over human AChE; up to 530-fold selectivity was achieved with carbamate 11d. A 3D QSAR model is presented that is reasonably consistent with log inhibition selectivity of 34 carbamates. Toxicity of these compounds to live Anopheles gambiae was demonstrated using both tarsal contact (filter paper) and topical application protocols. (C) 2012 Elsevier Ltd. All rights reserved.
Authors
I am an author on this paper
Click your name to claim this paper and add it to your profile.
Reviews
Recommended
No Data Available