AI Article Synopsis
- - A new series of compounds known as (6-aminopyridin-3-yl)(4-(pyridin-2-yl)piperazin-1-yl) methanone derivatives were discovered to selectively block the TRPV4 channel and reduce pain in animal models.
- - The research focused on enhancing a previously identified compound (16d) to develop a more effective compound (26i) that showed promising results.
- - The paper details the design, synthesis, and analysis of how the structure of these compounds relates to their effectiveness (structure-activity relationship or SAR).
Article Abstract
A novel series of (6-aminopyridin-3-yl)(4-(pyridin-2-yl)piperazin-1-yl) methanone derivatives were identified as selective transient receptor potential vanilloid 4 (TRPV4) channel antagonist and showed analgesic effect in Freund's Complete Adjuvant (FCA) induced mechanical hyperalgesia model in guinea pig and rat. Modification of right part based on the compound 16d which was disclosed in our previous communication led to the identification of compound 26i as a flagship compound. In this paper, we described the details about design, synthesis and structure-activity relationship (SAR) analysis at right and left part of these derivatives (Fig. 1).
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| http://dx.doi.org/10.1016/j.bmc.2017.02.047 | DOI Listing |
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