Investigation of 7-benzylidenenaltrexone derivatives as a novel structural antitrichomonal lead compound. Issue 21 (1st November 2015)

• Record Type: Journal Article
• Authors: Kutsumura, Noriki; Nakajima, Ryo; Koyama, Yasuaki; Miyata, Yoshiyuki; Saitoh, Tsuyoshi; Yamamoto, Naoshi; Iwata, Satoshi; Fujii, Hideaki; Nagase, Hiroshi
• Is Part Of: Bioorganic & medicinal chemistry letters. Volume 25:Issue 21(2015)
• Page Start: 4890
• Page End: 4892
• Publication Date: 2015-11-01
• Subjects: Trichomonas -- DOR -- BNTX -- Opioid -- Antagonist; Bioorganic chemistry -- Periodicals; Pharmaceutical chemistry -- Periodicals; 572
• DOI: 10.1016/j.bmcl.2015.06.002
• Languages: English
• ISSNs: 0960-894X

Abstract

Graphical abstract: Abstract: We evaluated antitrichomonal effects of δ opioid receptor (DOR) agonists and antagonists. Although all the agonists were inactive, the DOR antagonists BNTX (2a ) and its derivatives2b –d showed antitrichomonal activity with MIC of 20–40 μM. In addition, the development of a more effective synthetic method for the BNTX derivatives was achieved by using the Knoevenagel condensation.