Investigation of 7-benzylidenenaltrexone derivatives as a novel structural antitrichomonal lead compound

Bioorganic & Medicinal Chemistry Letters
2015.0

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 derivatives 2b-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.

Knowledge Graph

Similar Paper

Investigation of 7-benzylidenenaltrexone derivatives as a novel structural antitrichomonal lead compound
Bioorganic & Medicinal Chemistry Letters 2015.0
Antitrichomonal activity of δ opioid receptor antagonists, 7-benzylidenenaltrexone derivatives
Bioorganic & Medicinal Chemistry 2017.0
Opioid δ1 receptor antagonist 7-benzylidenenaltrexone as an effective resistance reverser for chloroquine-resistant Plasmodium chabaudi
Bioorganic & Medicinal Chemistry Letters 2011.0
Parallel methods for the preparation and SAR exploration of N-ethyl-4-[(8-alkyl-8-aza-bicyclo[3.2.1]oct-3-ylidene)-aryl-methyl]-benzamides, powerful mu and delta opioid agonists
Bioorganic & Medicinal Chemistry Letters 2004.0
Structure−Antitussive Activity Relationships of Naltrindole Derivatives. Identification of Novel and Potent Antitussive Agents
Journal of Medicinal Chemistry 2008.0
Discovery of a Potent and Efficacious Peptide Derivative for δ/μ Opioid Agonist/Neurokinin 1 Antagonist Activity with a 2′,6′-Dimethyl-<scp>l</scp>-Tyrosine: In vitro, In vivo, and NMR-Based Structural Studies
Journal of Medicinal Chemistry 2011.0
Synthesis of novel triplet drugs with 1,3,5-trioxazatriquinane skeletons and their pharmacologies. 1: Synthesis of triplet drugs with morphinan skeletons
Bioorganic &amp; Medicinal Chemistry Letters 2011.0
Conversion of the Potent δ-Opioid Agonist H-Dmt-Tic-NH-CH<sub>2</sub>-Bid into δ-Opioid Antagonists by N-Benzimidazole Alkylation<sup>1</sup>
Journal of Medicinal Chemistry 2005.0
Benzylideneoxymorphone: A new lead for development of bifunctional mu/delta opioid receptor ligands
Bioorganic &amp; Medicinal Chemistry Letters 2017.0
Aminotetralins as narcotic antagonists. Synthesis and opiate-related activity of 1-phenyl-1-aminotetralin derivatives
Journal of Medicinal Chemistry 1979.0