期刊
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
卷 24, 期 7, 页码 1711-1714出版社
PERGAMON-ELSEVIER SCIENCE LTD
DOI: 10.1016/j.bmcl.2014.02.049
关键词
Acetylcholinesterase; Reactivation; Cyclosarin (GF); GF-inhibited hAChE; Structure-activity relationship; Heteroaryl keto-oximes
资金
- Defense Threat Reduction Agency [HDTRA1-10-C-0041]
The goal of this research was to identify structurally novel, non-quaternarypyridinium reactivators of GF (cyclosarin)-inhibited hAChE that possess the capacity to mediate in vitro reactivation of GF-inhibited human acetylcholinesterase (hAChE). New compounds were designed, synthesized and assessed in GFinhibited hAChE assays. Structure activity relationships for AChE binding and reactivation of GF-inhibited hAChE were developed. Lead compounds from two different chemical series, represented by compounds 17 and 38, displayed proficient in vitro reactivation of GF- inhibited hAChE, while also possessing low inhibition of native enzyme. (c) 2014 Elsevier Ltd. All rights reserved.
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