期刊
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
卷 25, 期 20, 页码 4437-4440出版社
PERGAMON-ELSEVIER SCIENCE LTD
DOI: 10.1016/j.bmcl.2015.09.012
关键词
Flufenamic acid; Pentafluorosulfanyl group; Computational conformational analyses; Ion channel modulator; Bile acid-sensitive ion channel; AKR1C3 inhibitor
资金
- National Institutes of Health [P30-ES013508, P01-CA163227-03]
Pentafluorosulfanyl-containing analogs of flufenamic acid have been synthesized in high yields. Computationally, pK(a), LogP and LogD values have been determined. Initial bioactivity studies reveal effects as ion channel modulators and inhibitory activities on aldo-keto reductase 1C3 (AKR1C3) as well as COX-1 and COX-2. (C) 2015 Elsevier Ltd. All rights reserved.
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